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887 Cards in this Set

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Basic Pharmacokinetics
Way to increase the renal elimination of a weak acid
Alkalinize the urine
1. volumes of plasma, blood, ECF, total body water for 70 kg. person?
2. Eq. for Vd, half life, Cl, Infusion rate, loading dose, maintanence dose?
1. 3, 5, 12-14, 40-42

2. Vd=Dose/Conc. at time 0

half life=.7/k k=Cl/Vd it is the elimination constant

Cl=k x Vd or elimination rate/plasma conc.

Infusion rate (k0)=Cl x Steady state concentration

LD= V(d) x steady state conc.

MD= Cl x steady state conc. x dosing interval
Way to inc. the renal elimination of a weak base
Acidify the urine
1. Time to 50, 90, 95, 100 percent steady states?
2. What is the normal GFR?
1. 1x half life, 3.3x half life, 4-5x half life, >7 half life
2. 120 ml/min.
Weak acid % ionized at pH-pKa of -2,-1,0,1,2
1, 10, 50, 90, 99
List 4 phases of clinical testing?
1. small group volunteers w/o disease test safety. PHARMOCOKINETICS at different levels.
2. 100 or more pt. with disease COMPARE AGAINST PLACEBO to see effectiveness
3. 1000 or more pt. with disease compare with placebo. how well work with common SE. DOUBLE BLIND. Compare against gold standard.
4. out market. post market surveilance for AE. Less common and possible more severe toxicities. not rigidly regulated by FDA.
% weak base ionized at pH-pKa of -2, -1, 0, 1, 2
99, 90, 50, 10, 1
Time it takes for amount of drug to fall to half of its value, when is it constant, which kinetics? (majority of drugs)
Half-life (T1/2)
first order kinetics constant
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD) VD=dose/plasma level
Plasma concentration of a drug at a given time
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of administered dose of a drug that reaches systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination, # half lives it takes
Steady state: math=7, clinically 4-5
Measurement used to determine the safety and eficacy of generic drugs
This step of metabolism makes drug more hydrophilic and hence augments elimination
Phase I
Different steps of Phase I
Oxidation, reduction, hydrolysis
Inducers of Cytochrome P450 (CYP450)
Barbiturates, phenytoin, carbamazepine, and rifampin, ethanol, St. Johns Wart, isoniazid
Inhibitors of CYP450
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit, Adenavir, ethanol, Ritonavir
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
so put on glucuronic acid, acetic acid, sulfuric acid
Constant percentage of substrate metabolized per unit time, directly proportional to plasma conc.
First order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor, compare 2 which better
Affinity, closest to Y axis
Selectivity of a drug for its receptor
Amount of drug necessary to elicit a biologic effect, compare 2 which better
Potency, closest Y axis
Ability of drug to produce a biologic effect, compare two which better
Efficacy, maximal height of curve
A drug that will produce 100% of the maximum response regardless of the potency
Full agonist
Will produce less than 100% of the response
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind to either the same or different site as the drug
Noncompetitive antagonist
Mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
MOA utilizes transmembrane receptors
MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers and Acetylcholine
Median effective dose required for an effect in 50% of the population
Median toxic dose required for a toxic effect in 50% of the population
Dose which is lethal to 50% of the population
Window between therapeutic effect and toxic effect and equation
Therapeutic index TD50/ED50
Receptors linked to GS
B1, B2, D1
Receptors linked to Gq
M1, M3, a1
Receptors linked to Gi
M2, A2
Drug with a high margin of safety
High therapeutic index
Drug with a narrow margin of safety
Low therapeutic index
Antidotes and agents used in drug overdose
Antidote used for lead, arsenic, mercury poisoning
Dimercaprol, EDTA
a chelating agent
Antidote used for cyanide poisoning
Nitrites: convert Hgb to methgb which cyanides bind stronger to rather than cytochrome oxidase
Antidote used for anticholinergic poisoning
Physostigmine: cholinesterase inhibitor.
Antidote used for organophosphate/anticholinesterase poisoning (2)
Atropine(antimuscarinic), pralidoxime (reactivates inhibited acetylcholinesterase by breaking bond of insecticide and enzyme) (2-PAM)
Antidote used for iron salt toxicity
Deferoxamine, a chelating agent
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst), inc. glutathione, inhibits formation metabolite, directly interacts with metabolite
Antidote for arsenic, mercury, lead, and gold poisoning

Heavy metals act by chemically reacting with adjacent sulfhydryl residues on metabolic enzymes, creating a chelate complex that inhibits the affected enzyme's activity. Dimercaprol competes with the sulfhydryl groups for binding the metal ion, which is then excreted in the urine.
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine, a chelating agent or dimercaprol
Antidote used for heparin toxicity
Protamine sulfate, a base
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid, inhibits plasminogen activation

It binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin
Antidote used for methanol and ethylene glycol (2)
Ethanol, which has higher affinity for alcohol dehydrogenase.
Fomepizole: alcohol dehydrogenase inhibitor.
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil: a GABA receptor antagonist
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate to correct acidosis
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity. What if they have become arrythmic
Digibind: antibody fragments against digoxin (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Antidote for methotrexate toxicity
Leucovorin: Folinic acid is a 5-formyl derivative of tetrahydrofolic acid. It is readily converted to other reduced folic acid derivatives (e.g. tetrahydrofolate). Since it does not require the action of dihydrofolate reductase for its conversion, it will be unaffected by inhibition of this enzyme by drugs such as methotrexate.
Antidote for beta-blockers and hypoglycemia

Glucagon binds to the glucagon receptor, a G protein-coupled receptor located in the plasma membrane. The conformation change in the receptor activates G proteins, alpha subunit specifically activates the next enzyme in the cascade, adenylate cyclase.

Adenylate cyclase manufactures cAMP (cyclical AMP) which activates cAMP-dependent protein kinase. This enzyme in turn activates phosphorylase B kinase, which in turn, phosphorylates phosphorylase B. Phosphorylase B is the enzyme responsible for the release of glucose-1-phosphate from glycogen polymers

in heart can inc. cAMP without having to use Beta receptor
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate): it binds K+ in the gut
Antidote for salicylate intoxication
Alkalinize urine, dialysis
Cancer Chemotherapy
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Pyrimidine analog that causes "Thiamine-less death" given with leucovorin. Used for solid tumors.
5-flouracil (5-FU): When goes into cells converted into 5-fDUMP which blocks thymidylate synthase
Drug used in cancer therapy causes Cushing-like symptoms
Side effect of Mitomycin and MOA
SEVERE myelosuppression

Changed into alkylating agent so it crosslinks DNA to fight hypoxic tumors
MOA of cisplatin + use of
Alkylating agent. Used for bladder, lung, ovary, testis
Common toxicities of cisplatin
Nephro and ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation: INHIBITS purine metabolism. Used for acute leukemia.
6-mercaptopurine (6-MP): after HGPRTase metabolite inhibtis enzymes of purine synthesis
Interaction with this drug requires dose reduction of 6-MP
Allopurinol, because xanthine oxidase metabolized 6-MP
May protect against doxorubicin toxicity by scavenging free radicals and MOA of doxorubicin
Dexrazoxane: inhibitor of iron mediated free radical generation to protect against cardiotoxicity.

It intercalates between base pairs, inhibitis topoisomerase II, generates free radicals
Breaks DNA via free redicals, Used for Hodgkins, squamous cell, testicular. What is the drug and what is limiting SE?
limiting SE is pulmonary fibrosis.
This regimen if used for testicular cancer produces near 100% response
Bleomycin (free radicals) +vinblastine (prevent microtubule assembly)+etoposide (inc. degradation DNA via topo II and inhibts electron transport)+cisplatin (alkylating) produce almost a 100% response when all agents are used for this neoplasm
MOPP regimen used in Hodgkin's disease (HD) + MOA of each

How each work?
Mechlorethamine (alkylating agent) + oncovorin (vincristine) (prevent assembly of microtubles) + procarbazine (forms hydrogen peroxide=free radicals and a alkylating agent), and prednisone
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) (intercalates between bases of DNA) +bleomycin (free radicals), vinblastine (prevents formation of microtubules) +dacarbazine (alkalating agent)
Regimen used for non-Hodgkin's lymphoma
COP (cyclophosphamide (alkylating agent), oncovorin(vincristine, prevents formatoin of microtubules), and prednisone)
Regimen used for breast cancer
CMF (cyclophosphamide (alkylating agent), methotrexate (inhibits dihydrofolate reductase), and fluorouracil (thiamine less death) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation.
What cancer used for?
Mechlorethamine: spontaneously converts in body to reactive cytotoxic product.

Hodgkin disease
Anticancer drug also used in RA, SE is hemorrhagic cystitis. What cancers used for? what is this SE due to and how can you prevent it?
non hodgkin, ovary, breast

Cyclophosphamide: The main effect of cyclophosphamide is due to its metabolite phosphoramide mustard. This metabolite is only formed in cells which have low levels of ALDH.

Phosphoramide mustard forms DNA crosslinks between and within DNA strands. This leads to cell death.

SE due to acrolein formation in the kidney. Give hydration and MESNA
Prevention of cyclophosphamide induced hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA): Mesna assists to neutralise these metabolites by binding through its sulfhydryl-moieties, and also increases urinary excretion of cysteine.
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation. Used for acute leukemia, lymphomas, Kaposi, neuroblastoma, testicular.
Vincristine and vinblastine
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase. Advanced breast and ovarian cancer.
Paclitaxel (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Agent similar to cisplatin, less nephrotoxic, but what at more risk for?

Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
Used for hairy cell leukemia; MOA
Interferon alpha
activates NK cells
Anti-androgen used for prostate cancer
Flutamide (Eulexin): androgen receptor antagonist
Anti-estrogen used for estrogen receptor + breast cancer
SERM used only for metastatic breast cancer. No risk of endometrial cancer.
Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
Anti-emetics used in association with anti-cancer drugs. How do they work?
Odansetron, granisetron

They are 5-HT3 (serotonin receptor subtype ) antagonist
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU) and lomustine (CCNU): alkylating agents
Produces disulfiram-like reaction with ethanol, also blocks MAO
Procarbazine: alkylating agent also forms hydrogen peroxide generating free radicals
Endocrine drugs: hypothalamic and pituitary hormones
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
Somatotropin (GH) analog used in GH deficiency (dwarfism)
GHRH analog used as diagnostic agent
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively Name 2.
Leuprolide or goserelin
GnRH antagonist with more immediate effects, used for infertility
Ganirelix, to prevent premature LH surge. Also cetrorelix.
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Name 3
Bromocriptine or pergolide or Cabergoline

Pergolide is in decreasing use, as it has been associated with fibrotic heart disease since 2003 [1]. This problem is thought to be due to pergolide's action at the 5-HT2B serotonin receptors of cardiac myocytes
Hormone inhibiting prolactin release
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
Thyroid and anti-thyroid drugs
Most widely used thyroid drugs contain this thyroid hormone. Name 2.
L-thyroxine (T4)
Synthroid and Levoxyl
T3 compound less widely used

Unlike synthroid, cytomel results in a rapid elevation in thyroid hormone levels that result in supraphysiological levels 2 to 6 hours after ingestion and a rapid clearance.
Anti-thyroid drugs
Thioamides, iodides, radioactive iodine, and ipodate
Thioamide agents used in hyperthyroidism
Methimazole and propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
PTU (propylthiouracil) MOA
does PTU affect the iodide transporter in and if not who could
PTU inhibits many steps in the synthesis of thyroid hormones, including the addition of iodide to thyroglobulin by the enzyme thyroperoxidase, a necessary step in the synthesis of thyroxine, and by inhibiting the enzyme 5'-deiodinase which converts T4 to T3.

PTU does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate.
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radioactive iodine
Radio contrast media that inhibits the conversion of T4 to T3
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3 in peripheral how?
Beta-blockers such as propranolol

via 5' deiodinase
Adrenocorticosteroid and adrenocortical antagonists
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Pneumonic for 3 zones of adrenal cortex
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Short acting GC's
Cortisone and hydrocortisone (equivalent to cortisol)
Intermediate acting GC's (4)
Prednisone, methylprednisolone, prednisolone, and triamcinolone
Long acting GC's
Betamethasone, dexamethasone, and paramethasone
Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
Period of time of therapy after which GC therapy will need to be tapered
5-7 days
Inhibitors of corticosteroids biosynthesis
Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test + MAO of drug
Metyrapone: Metyrapone blocks cortisol synthesis by inhibiting 11B hydroxylase. this stimulates ACTH secretion, which in turn increases plasma 11- deoxycortisol levels. When excess ACTH secretion is the cause of hypercortisolism, the metyrapone test helps clarify if the source of the ACTH is pituitary or ectopic (non-pituitary).
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Since cortisol helps break down muscle, aminoglutethimide is used by bodybuilders in a steroid cycle.
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Antiprogestin used as potent antagonist of GC receptor
Diuretic used to antagonize aldosterone receptors
Common SE of spironolactone
Gynecomastia and hyperkalemia
Gonadal hormones and inhibitors
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Antiestrogen drug used for fertility
antiestrogen drug used for breast cancer
Clomiphene (acts by inhibiting the action of estrogen on the gonadotrope cells in the anterior pituitary gland "Sensing" low estrogen levels, follicle-stimulating hormone (FSH) release is increased, leading to a higher rate of ovulation ) and tamoxifen
Common SE of tamoxifen and raloxifene
Hot flashes
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
Diethylstilbestrol (DES)
Estrogen mostly used in oral contraceptives (OC) (2)
Ethinyl estradiol and mestranol which is metabolized to ethinyl estradiol
Anti-progesterone used as abortifacient
Mifepristone (RU-486)
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
Combination oral contraceptives (OC)
Oral contraceptive available in a transdermal patch
Converted to more active form DHT and by what enzyme?
Testosterone: 5 alpha reductase
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
Finasteride (Proscar and Propecia respectively)
Anabolic steroid that has potential for abuse
Nandrolone and stanozolol
Anti-androgen used for hirsutism in females (2)
Cyproterone acetate or Spironolactone
Drug is used with testosterone for male fertility
Leuprolide: GnRH agonist
Pancreatic hormones, antidiabetics, and hyperglycemics
Alpha cells in the pancreas
Produce glucagon
Beta cells in the pancreas
Produce insulin
Beta cells are found. What type of compounds can increase the release of its product?
Islets of Langerhans

Increased by glucose, sulfonylureas, M-activators, B2 agonists
**Decreased by alpha 2 agonist
Delta cells in the pancreas
Produce Somatostatin
Product of proinsulin cleavage used to assess insulin abuse
Exogenous insulin
Little C-peptide
Lab measurement to determine source of insulin.
Very rapid acting insulin, having fastest onset and shortest duration of action. Describe peak, duration
Lispro (Humalog)

Peaks at 15-30 minutes and duration is 3-4 hours
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia? Peak and duration? How treat diabetic ketoacidosis?
Regular (Humulin R): Peak 30 min - 3 hours duration 5-7 2-4 min. IV,

Regular IV, fluids and electrolytes
Long acting insulin
Ultralente (humulin U)
onset 3-4 hr, peak 8-16 hr, dur. 24-36 hr.
Ultra long acting insulin, has over a day duration of action
Glargine (Lantus): has no peak and works greater 24 hr
Major SE of insulin
Receptor for glucose found in the liver and pancreas and kidney

Describe the other receptors

3=neurons, placenta
4=muscle and adipose
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
Examples of alpha-glucosidase inhibitors (AGI)
Acarbose, miglitol
MOA of AGI's
Act on intestine, delay absorption of glucose
SE of AGI's. What do you not want to give these pt.?
Flatulence (do not use beano to tx, Beano is an enzyme-based dietary supplement that is alleged by its manufacturer to reduce gas in the digestive tract, thereby preventing flatulence. It contains the enzyme alpha galactosidase. It is claimed that the human digestive tract does not contain alpha galactosidase; however acarbose may work against alpha galactosidase ), diarrhea, abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's
Amino acid derivative with MOA similar to sulfonylureas but a shorter DOA
Nateglinide, a phenylalanine derivative
MOA of nateglinide
Insulin secretagogue, closes K+ channels causing depolarization
The only biguanide approved for treating type 2 diabetes?
Drugs available in combination with metformin (4)
Glyburide, glipizide, and rosiglitazone, and pioglitazone
MOA of metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity. Works via gene expression.
Most important potential SE of metformin
Lactic acidosis due to more glucose uptake by the cells. By blocking gluconeogenesis may impair hepatic metabolism of lactic acidosis esp. with renal insufficiency
Name a Meglitinide and use of.
Repaglinide: use just before meals due to short half life.
Also Nateglinide.
MOA of repaglinide
Insulin release from pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the beta cells. This depolarizes the beta cells, opening the cells' calcium channels, and the resulting calcium influx induces insulin secretion.; faster and shorter acting than sulfonylurea
First generation sulfonylureas. Which is ok with renal dysfunction? Which is most potent?
Chlorpropamide (most potent), tolbutamide (ok with renal dysfunction), tolazamide, Acetohexamide.
Second generation sulfonylureas. Which is dec. in dose with renal problems. Which with hepatic problems?
Glyburide (dec. with renal), glipizide (dec. with hepatic), glimepiride, etc.
MOA of both generations
Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide
Sulfonylurea NOT recommended for elderly because of very long half life
Name three Thiazolidinediones
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Reason troglitazone was withdrawn from market
Hepatic toxicity
MOA of thiazolindinediones
Stimulate PPAR-gamma receptor involved in transcription in insulin responsive genes. Senstitizes target tissues to insulin.
SE of Thiazolindinediones
Edema, mild anemia; interaction (they are inducers) with drugs that undergo CytP450 3A4 metabolism
Hyperglycemic agent to treat low serum glucose that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Drugs used in bone homeostasis
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid

MOA of Bisphosphonates
Inhibits osteoclast bone resorption and stabalize hydroxyapatite structure
Only bisphosphonates available IV
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
**Alendronate DOC with HRT or for steroid induced osteoperosis
Major SE of bisphosphonates
Chemical esophagitis esp. with alendronate when pt. has inadequate water intake
1. Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
2. Recombinant DNA PTH analog used used one time daily to stimulate osteoblasts. Name drug and major SE?
1.Etidronate and Pamidronate
2. Teriparatide, with continous infustion stimulates osteoclasts. Also used more 2 years inc. risk of osteosarcoma.
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CA tx.
Raloxifene (SERM-selective estrogen receptor modulator)
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
Used especially in postmenopausal women, dosage should be 1500 mg
Vitamin given with calcium to ensure proper absorption
Vitamin D
Drugs with important actions on smooth muscle
Disease caused by excess ergot alkaloids
St. Anthony's Fire: The symptoms can be roughly divided into convulsive symptoms and gangrenous symptoms.
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids: local hormones made many places, not just endocrine glands. Formed by the tissues where they act.
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
Endogenous Drug that causes contraction of the uterus
Distribution of histamine receptors H1, H2, and H3
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
Prototype antagonist of H1 and H2 receptors respectively
Diphenhydramine and impromidine or cimetidine respectively
1st generation antihistamine that is highly sedating
1st generation antihistamine that is least sedating (2)

Name all 1st generation antihistamines
Chlorpheniramine or cyclizine

Chlorpheniramine, cyclizine, diphenydramine, dimenhydrinate, doxepin, doxylamine, hydroxyzine, meclizine, promethazine
2nd generation antihistamines, name 3
Fexofenadine, loratadine, and cetirizine
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)

H1 receptor antagonist and piperazine derivative used primarily as an antihistamine for the treatment of itches and irritations, an antiemetic for the reduction of nausea, as a weak analgesic and as an anxiolytic. Good for people with drug abuse who have anxiety.
H1 antagonist used in motion sickness (5)
Dimenhydrinate, Diphenhydramine, cyclizine, meclizine, hydroxyzine
Most common side effect of 1st generation antihistamines
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been removed from the market)
H2 blocker that causes the most interactions with other drugs
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Receptors for serotonin are located. How do they work? MOA?
5 HT-1D : Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance

5 HT-2 : Smooth muscle and platelets.

5 HT-3 : CNS. chemoreceptor area and vomiting center.
5HT-1d agonist used for migraine headaches (3)
Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation
1.H1 blocker that is also a serotonin antagonist, what used for?

2. Two serotonin antagonists that have alpha 1 blocking properties?

antihistaminic and antiserotonergic agent. It acts as a 5-HT2 receptor antagonist and also blocks calcium channels.

Cyproheptadine is used in the treatment of allergies (specifically Hay fever) and is also used to stimulate appetite in underweight people (e.g. anorexia nervosa).

Cyproheptadine may also be used to combat SSRI-induced sexual dysfunction, but is used cautiously in this manner due to the fact that it may reverse the effects of the SSRI.

Cyproheptadine is also used for the treatment of Cushing's Syndrome, the treatment of serotonin reactions secondary to meperidine, and may be used, though rarely, as a prophylactic drug for migraine headaches.

2. Ketanserin and Phenoxybenzamine
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction (3)
Ketanserin, cyproheptadine, phenoxybenzamine and ergot alkaloids (partial agonist of alpha and serotonin receptors)
Ergot Alkaloids
1. agent used for postpartum bleeding
2. agents for migraines, one for acute, one for prophylaxis
1. ergonovine
2. acute=ergotamine: alpha VC
prophylaxis=methysergide or ergonavine
Serotonin or ergots:
Agents used in treatment of carcinoid tumor
Ketanserin cyproheptadine, and phenoxybenzamine (all HT-2 antagonist) + methysergide
Serotonin antagonist used in chemotherapeutic induced emesis and which receptor do they work on? (4)
Ondansetron, granisetron, dolasetron and alosetron
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease

5 HT-3 antagonist Associated with fatal bowel complications

DOC of chemo induced nausea and vomiting
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside: counteracts the alpha and HT VC of the ergot alkaloids
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE of ergot alkaloids
Hallucinations resembling psychosis (LSD), others see GI distress and prolonged vasoconstriction
Ergot alkaloid used as an illicit drug

Partial dope agonist and The hallucinogenic effects of LSD are attributed to its strong partial agonist effects at 5-HT2A receptors as specific 5-HT2A agonist drugs are hallucinogenic and largely 5-HT2A specific antagonists block the hallucinogenic activity of LSD.[14] Exactly how this produces the drug's effects is unknown, but it is thought that it works by increasing glutamate release and hence excitation in the cortex, specifically in layers IV and V
Dopamine agonist used in hyperprolactinemia
Peptide causing increased capillary permeability and edema (2)
Bradykinin and histamine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Drug causing depletion of substance P (vasodilator)
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
Difference between COX 1 and COX 2 "
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
3 Drugs that selectively inhibits COX 2
Celecoxib, valdecoxib, and rofecoxib
Inhibitor of lipoxygenase that can help treat asthma
Zileuton: selective and specific inhibitor of 5-lipooxygenase
Major SE of zileuton
Liver toxicity
Inhibitor of leukotrienes (LTD4) receptors and used in asthma prophylaxis
Zafirlukast and montelukast
Used in pediatrics to maintain patency of ductus arteriosis
Prostaglandin Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)

Prostacyclin acts chiefly to prevent platelet formation and clumping involved in blood clotting. It is also an effective vasodilator.
Prostaglandin used in the treatment impotence
Alprostadil (PGE1)
Irreversible, nonselective COX inhibitor
Class of drugs that reversibly inhibit COX
Primary endogenous substrate for Nitric Oxidase Synthase
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
mechanism: cGMP facilitates the dephosphorylation and inactivation of myosin light chains
Long acting beta 2 agonist used in asthma (2)
Salmeterol and Formoterol
Muscarinic antagonist used in asthma for people unable to tolerate adrenergic agonists. (2)
Ipratropium and Tiotropium
MOA action of cromolyn
Mast cell stabilizer
Enzyme which theophylline inhibits
Phosphodiesterase this leads to an inc. of cAMP which causes smooth muscle dilation
Methylxanthine derivative used as a remedy for intermittent claudication
Antidote for severe CV toxicity of theophylline
Beta blockers
MOA of corticosteroids"
inhibit phospholipase A2
SE of long term (>5 days) corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
MOA of quinolones
Inhibit Topoisomerase II (DNA gyrase) blocking relaxation of supercoiled DNA. Also block Topo 4 which is required for DNA seperation.
MOA of penicillin
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
Drug used for MRSA
Vancomycin MOA
Blocks peptidoglycan synthesis, the D-ala-D-ala pentapeptide linkage
Type of resistance found with vancomycin
Point mutation: Terminal D-ala replaced by D-lactate
N. Meningitidis prophylaxis in exposed patients and drug MOA
Rifampin: inhibits DNA-dependent RNA polymerase
Technique used to diagnose perianal itching, and the drug used to treat it. MOA of drug
Scotch tape technique and mebendazole (selectively inhibits microtubule synthesis and glucose uptake in nematodes)
Two toxicities of aminoglycosides
nephro and ototoxicity
DOC for Legionnaires' disease
Complete MOA of sulfonamides
Competes with PABA, Inhibiting dihydropteroate synthase

PABA uses dihydropteroate synthase to go to dihydrofolic acid. This uses dihydrofolate reductase to go to tetrahydrofolic acid. This is used to make purines
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC of otitis media and backup drug for Lyme disease
Class of antibiotics that have 10% cross sensitivity with penicillins
PCN active against pseudomonas
Carbenicillin, piperacillin and ticarcillin
Antibiotic causing red-man syndrome, and prevention
Vancomycin, infusion at a slow rate and antihistamines
Drug causes teeth discoloration
MOA of tetracycline
Decreases protein synthesis by inhibiting 30S ribosome
Drug that causes gray baby syndrome and aplastic anemia
Chloramphenicol (50S)
Drug notorious for causing pseudomembranous colitis
Clindamycin (50S)
DOC for tx of pseudomembranous colitis + MOA
Metronidazole: good for anaerobes

Metronidazole is selectively taken up by anaerobic bacteria and sensitive protozoal organisms because of the ability of these organisms to reduce metronidazole to its active form intracellularly. The nitro group of metronidazole is chemically reduced by ferredoxin (or ferredoxin-linked metabolic process) and the products are responsible for disrupting the DNA helical structure, thus inhibiting nucleic acid synthesis
Treatment of resistant pseudomembranous colitis
ORAL vancomycin: It is a large hydrophilic molecule which partitions poorly across the gastrointestinal mucosa
Anemia caused by trimethoprim
Megaloblastic anemia: it may inhibit dyhdrofolate in humans also
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
Name 4 bugs that metronidazole is the DOC for?
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
Treatment for TB patients
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol

I saw a red pyre burning the liver
Metronidazole SE if given with alcohol and mechanism
Disulfiram-like reaction because it inhibits acetaldehyde dehydrogenase
Common side effect of Rifampin
Red urine discoloration: metabolites are red-orange color
MOA of nystatin
nystatin binds to ergosterol, a major component of the fungal cell membrane. When present in sufficient concentrations, it forms pores in the membrane that lead to K+ leakage and death of the fungus
Neurotoxicity with isoniazid (INH) prevented by
Administration of Vit. B6 (pyridoxine) as this drug inc. excretion of pyridoxine in slow acetylators
Toxicity of amphotericin
SE seen only in men with administration of ketoconazole
Gynecomastia because it blocks steroid synthesis
Topical DOC in impetigo + MOA
Topical mupirocin (Bactroban)

It has a unique mechanism of action, which is selective binding to bacterial isoleucyl-tRNA synthetase, which halts the incorporation of isoleucine into bacterial proteins. Because this mechanism of action is not shared with any other antibiotic, mupirocin has few problems of antibiotic cross-resistance
DOC for influenza A
Amantadine: prevents uncoating of influenza A

The drug interferes with a viral protein, M2 (an ion channel), which is needed for the viral particle to become "uncoated" once it is taken inside the cell by endocytosis.
Ribavirin: inhibits viral RNA polymerase
DOC for CMV retinitis
Ganciclovir: block RNA polymerase of virus
SE for ganciclovir
Neutro, leuko and thrombocytopenia
Anti-viral agents associated with Stephen Johnson syndrome
Nevirapine, amprenavir
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Protease inhibitors
Antivirals that are teratogens
Delavirdine, efavirenz, and ribavirin
Antivirals associated with neutropenia
Ganciclovir, zidovudine, saquinavir, and interferon
HIV med used to reduce transmission during birth
AZT (zidovudine)
Drug used for African sleeping sickness
Drug used in Chagas disease
Nifurtimox: T cruzi lacks catalase and this drug makes oxygen free radicals
Cephalosporins able to cross the BBB
Cefixime (2nd) and 3rd generation
Drug used for N. gonorrhea in females
Ceftriaxone because most gonorrhea resistant to penicillin
Cephalosporin causes kernicterus in neonates
Ceftriaxone or cefuroxime; these may cause hemolytic anemia
SE of Isoniazid
Peripheral neuritis due to pyridoxine deficiency and hepatitis due to toxic metabolite
Aminoglycoside that is least ototoxic
Drug used in exoerythrocytic cycle of malaria
Oral antibiotic of choice for moderate inflammatory acne
Drug of choice for leprosy and MOA
Dapsone: PABA antagonist to inhibit folate synthesis.
DOC for herpes and its MOA

It is selectively converted into a monophosphate form by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, aciclo-GTP, by cellular kinases. Aciclo-GTP is a very potent inhibitor of viral DNA polymerase; it has approximately 100 times higher affinity to viral than cellular polymerase. Its monophosphate form also incorporates into the viral DNA, resulting in chain termination
Anti-microbials that cause hemolysis in G6PD-deficient patients
MOA of erythromycin
Inhibition of protein synthesis at the 50s subunit of ribosome
Anti-biotic frequently used for chronic UTI prophylaxis and MOA
sulfamethoxazole/ trimethoprim

sulf inhibits incorporation of PABA into folic acid, tri prevents reduction of dihydrofolate to tetrahydrofolate. Both excreted in urine.
Lactam that can be used in PCN allergic patients
SE of imipenem
What drug should you combine with this?
Anti-viral with a dose limiting toxicity of pancreatitis
Sedative Hypnotics
Common side effect of hypnotic agents
Occurs when sedative hypnotics are used chronically or at high doses
The most common type of drug interaction of sedative hypnotics with other depressant medications
Additive CNS depression
Name Benzodiazepines (8)
Diazepam, Alprazolam, chlordiazepoxide, clonazepam, flurazepam, lorazepam, oxazepam, triazolam
Major effect of benzodiazepines on sleep at high doses
REM is decreased
Neurologic SE of benzodiazepines
Anterograde amnesia: why at high doses can be used as date rape drug
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
Main route of metabolism for benzodiazepines
Benzodiazepines (3) that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
MOA for benzodiazepines (key word)
increase the FREQUENCY of GABA-mediated chloride ion channel opening
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil: benzodiazepine receptor antagonist
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
Benzodiazepine that is used for anesthesia. It is the shortest acting benzo.
Name two drugs useful with status epelepticus. Which one is the preffered agent for a child with a febrile seizure?
Diazepam and Lorazapam
Two Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
Agents having active metabolites, long half lives, and a high incidence of adverse effects (4)
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
Name 5 Barbiturates
Phenobarbital, Amobarbital, Pentobarbital, Secobarbital, thiopental
Barbiturates may precipitate this hematologic condition
Acute intermittent porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Liver enzyme INDUCTION
Barbiturates MOA KEY WORD
Increase the DURATION of GABA-mediated chloride ion channels
Barbiturate used for the induction of anesthesia
Important drug interaction with chloral hydrate
May displace coumadin from plasma proteins
Site of action for zaleplon and zolpidem and their advantage
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines). Bind more specifically to this receptor. Cause less daytime impairment and do not effect sleep as much.
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
Agent that is a partial agonist for the 5-HT1A receptor but that may not be reason it helps you sleep
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Two systems that will metabolize ethanol
metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Is ethanol first order or zero order
Zero order
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
System that increases in activity with chronic exposure and may contribute to tolerance
Agent that metabolize acetaldehyde to acetate
Aldehyde dehydrogenase
Agents that inhibit aldehyde dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
The most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
Agent that is teratogen and causes a fetal syndrome
Agent that is the antidote for methanol overdose
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Name Anti seizure Drugs by seizure type and back up drugs
1. TC and Partial = carbamazepine, phenytoin, valproic acid
2. abcense = ethosuximibe, valproic acid, clonazepam
3. myoclonic = valproic acid, clonazepam
4. back up = felbamate, gabapentin, lamotrigine, phenobarbital, tiagabine, topiramate,
Most frequent route of metabolism
Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
Sodium blockade in neuron = prolongation of inactivated state of Na+ channel
MOA for benzodiazepines and barbiturates
GABA-related targets
MOA for Ethosuximide
T type Calcium channels esp. in thalamic neurons that act as pacemakers
MOA for Valproic acid at high doses
Affect calcium, potassium, and sodium channels
Three Drugs of choice for generalized tonic-clonic and partial seizures
Valproic acid and Phenytoin and Carbamezepine
DOC for seizures in infants
Drugs of choice for absence seizures
Ethosuximide and valproic acid
Drug of choice for myoclonic seizures
Valproic acid
Drugs of choice for status epilepticus
IV diazepam or phenytoin (for prolonged therapy not acute)
Drugs that can be used for infantile spasms
Anti-seizure drugs used also for bipolar affective disorder (BAD) (4)
Valproic acid, carbamazepine, phenytoin and gabapentin
Anti-seizure drug of choice used also for Trigeminal neuralgia
Anti-seizure drugs used also for pain of neuropathic orgin
ex. postherpetic neuralgia
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
SE of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
Valproic acid
Laboratory value required to be monitored for patients on valproic acid
Serum ammonia and LFT's
SE for Lamotrigine
Stevens-Johnson syndrome
SE for Felbamate
Aplastic anemia and acute hepatic failure
Anti-seizure medication also used in the prevention of migraines
Phenytoin and Gabapentin
Antiseizure medicine that may cause agranulocytosis
Anti-seizure drugs used as alternative drugs for mood stabilization (4)
Carbamazepine, gabapentin, phenytoin, and valproic acid
General Anesthetics: inhaled and IV
Halothane, Enflurane, desflurane, isoflurane, sevoflurane, nitrous, theopental, fentanyl, propofol, midazolam, ketamine, etomidate
MOA of general anesthetics
Unclear, thought to increase the threshold for firing of CNS neurons
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC): alveolar conc. req to eliminate the response to a painful stimuli in 50% of pt.
2 Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Halothane and methoxyflurane
Most inhaled anesthetics SE
Decrease arterial blood pressure
Inhaled anesthetics are myocardial depressants
Enflurane and halothane
Inhaled anesthetic causes peripheral vasodilation
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Nitrous oxide
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous oxide
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene: prevents release of calcium from sarcoplasmic reticulum
IV barbiturate used as a pre-op anesthetic
Benzodiazepine used adjunctively in anesthesia
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Local Anesthetics
ester: tetracaine, procaine, benzocaine, cocaine
amides: bupivacaine, ropivacaine, lidocaine, prilocaine
MOA of local anesthetics (LA's)
Block voltage-dependent sodium channels
This may enhance activity of local anesthetics
This may antagonize activity of local anesthetics
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
Longer acting local anesthetics which are less dependent on vasoconstrictors
Tetracaine and bupivacaine
These LA's have surface activity
Cocaine and benzocaine
Most important toxic effects of most local anesthetics
CNS toxicity
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
LA causing methemoglobinemia
Skeletal Muscle Relaxants
depolarizing: succinylcholine
non: tubocurarine, pancuronium, vecuronium, atracurium, mivacurium
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
Nondepolarizing type antagonists
Agent with long duration of action and is most likely to cause histamine release
Non-depolarizing antagonist has short duration x2. Why?
Mivacurium: because it is metabolized by plasma cholinesterase
Atracurium: Hoffman
Agent can block cardiac muscarinic receptors
Agent undergoing Hofmann elimination (breaking down spontaneously)
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis. SE?
Succinylcholine: causes muscle pain postoperatively and myoglobinuria may occur
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Cholinesterase inhibitors
Spasmolytic drugs
diazepam, baclofen, cyclobenzaprine, dantrolene, tizanidine, botulinum,
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
Spasmolytic drugs
Spasmolytic drug that Facilitates GABA presynaptic inhibition
GABA agonist in the spinal cord
Similar to clonidine and may cause hypotension
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
Agent used for acute muscle spasm
Drugs Used in Parkinsonism & Other Movement Disorders
levodopa, benztropine, selegiline, trihexyphenidyl, amantadine, pergolide, bromocriptine, pramipexole, entacapone
What drugs can cause drug induced Parkinsonism?
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
This is combined with L-dopa, and mechanism of.

inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
Clinical response that may fluctuate in tx of Parkinson's dx
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
2 Ergot alkaloids that is are used for patients who are refractory or cannot tolerate levodopa, Common SE?
Bromocriptine or Pergolide: work at D2 agonist
Erythromelalgia: a rare disorder in which blood vessels, usually in the extremities and especially in the feet, are blocked and inflamed, causing a painful burning and throbbing sensation and red skin
Non ergot dopamine receptor agonists agents used as first-line therapy in the initial management of Parkinson's
Pramipexole and ropinirole
Enhances dopaminergic neurotransmission. SE's include CNS excitation, acute toxic psychosis and livedo reticularis
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
Entacapone and Tolcapone
2 Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on what?. Atropine-like side effects
Benztropine or trihexyphenidyl both antimuscarinics

Little effect on bradykinesia
Agent effective in physiologic and essential tremor
Agents used in Huntington's Disease
Tetrabenazine + reserpine (both amine depleting drug), Haloperidol (antipsychotic that is a dopamine receptor antag.)
Agents used in Tourette's dx and why they work
Haloperidol or pimozide
both block dopamine 2 receptor
Chelating agent used in Wilson's disease
older: haloperidol, chlorpromazine, fluphenazine, tribluoperazine, thioridazine
newer: clozapin, olanzapine, quetiapine, risperidone, ziprasidone
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Older antipsychotic agents, D2 receptors
Side effects occuring in antipsychotics that block dopamine
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
Antipsychotics that reduce positive symptoms only
Older antipsychotics
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
Clozapine, Risperidone, Olanzapine, aripiprazole, and sertindole
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
Atypical antipsychotic causing high prolactin levels
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
Drug used in neuroleptic malignant syndrome
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
Muscarinic blockers
Antipsychotic having the strongest autonomic effects
Antipsychotic having the weakest autonomic effects
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis
Anti-psychotic not shown to cause tardive dyskinesia
Anti-psychotics available in depot preparation
Fluphenazine and haloperidol
Reduced seizure threshold
Low-potency typical antipsychotics and clozapine
Orthostatic hypotension and QT prolongation
Low potency older agents (esp ziprasidone) and risperidone
Increased risk of developing cataracts
Major route of elimination for Lithium
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
Lithium toxicity
Drug increases the renal clearance hence decreases levels of lithium
Lithium is associated with this congenital defect
Cardiac anomalies and is contraindicated in pregnancy or lactation
DOC for bipolar affective disorder
SE of lithium
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
TCA: amytriptyline, doxepin, nortriptyline, imipramine, clomipramine, desipramine
SSRI: paroxetine, fluoxetine, sertraline, fluvoxemine, citolapram,
Heterocyclics: 2= maprotiline, buproprion, trazadone, amoxapine 3=mirtazapine, venlafaxine, nefazadone
MAO : moclobemide, isocarboxazid, phenelzine, tranylcypromine
Example of three antidepressants that are indicated for obsessive compulsive disorder
Clomipramine, fluoxetine and fluvoxamine
Neurotransmitters affected by the action of antidepressants
Norepinephrine and serotonin
Usual time needed for full effect of antidepressant therapy
2 to 3 weeks
Population group especially sensitive to side effects of antidepressants
Elderly patients
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
Side-effect profile and prior pt response
Well-tolerated and are first-line antidepressants (3)
SSRI's, bupropion, and venlafaxine
Monoamine oxidase inhibitors (MAOI)
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
Monamine oxidase inhibitors
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
Hypertensive crisis
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
Serotonin syndrome: muscle rigidity, myoclonus, hyperthermia, cardio instability, seizures
Tricyclic antidepressants (TCA)
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
Tricyclic antidepressants (TCA)
Three C's associated with TCA toxicity
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
Agents having higher sedation and antimuscarinic effects than other TCA's
Tertiary amines: amitriptyline and doxepin
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
TCA used in chronic pain, enuresis, and ADD
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
Secondary amines that have less sedation and more excitation effect
Nortriptyline, Desipramine
Antidepressant associated with neuroleptic malignant syndrome
2 Antidepressant associated with seizures and cardiotoxicity
Maprotiline + amoxapine
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
Antidepressant also used for sleep that causes priapism
2 Antidepressants which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
Nefazodone + venlafaxine
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
SE of mirtazapine
Liver toxicity, increased serum cholesterol
sedation and WG
Selective serotonin reuptake inhibitors (SSRI)
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
Citalopram and its metabolite escitalopram
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
SSRI indicated for premenstrual dysphoric disorder
Fluoxetine (Sarafem)
Some of SSRIs' therapeutic effects beside depression (name 5 others)
Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD
SSRI's less likely to cause a withdrawal syndrome
Opioid Analgesics & Antagonists
agonists: morphine, fentanyl, heroin, methadone, meperidine, codeine, oxycodone, propoxyphene
mixed: buprenorphine, nalbuphine, pentazocine
antagonists: naloxone, naltrexone, nalmefene
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
Ascending pathways
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
Presynaptic mu, delta, and kappa receptors
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
Postsynaptic Mu receptors
Tolerance to all effects of opioid agonists can develop except
Miosis and constipation
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
Name SE of opioid analgesics?
Name 10!
dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
Strong opioid agonists
Morphine, methadone, meperidine, and fentanyl
Opioids used in anesthesia
Morphine and fentanyl
Opioid used in the management of withdrawal states
Opioid available trans-dermally
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
Moderate opioid agonists
Codeine, hydrocodone, and oxycodone
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
Partial agonist or mixed antagonists

mixed=pentazocine, nalbuphine, butorphanol
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
Opioid antagonist that is given IV and had short DOA
Opioid antagonist that is given orally in alcohol dependency programs
These agents are used as antitussive
Dextromethorphan, Codeine
These agents are used as antidiarrheal
Diphenoxylate, Loperamide: Loperamide is an opioid receptor agonist and acts on the μ-opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids.
Drugs of Abuse
Inhalant anesthetics
NO, chloroform, and diethyl ether
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
Fluorocarbons and Industrial solvents
found in gasoline, paint thinner, glues, cements
Cause dizziness, tachycardia, hypotension, and flushing
Organic nitrites such as amyl nitrite, isobutyl nitrite "poppers"
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
Opioid Analgesics
5 Most commonly abused in health care professionals
Heroin, morphine, oxycodone, meperidine and fentanyl
This route is associated with rapid tolerance and psychologic dependence
IV administration
Leads to respiratory depression progressing to coma and death
Overdose of opioids
Describe abstinence syndrome of the opoids
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
Treatment for opioid addiction
Methadone, followed by slow dose reduction
This agent may cause more severe, rapid and intense symptoms to a recovering addict
Sedative-Hypnotics action
Reduce inhibition, suppress anxiety, and produce relaxation
Additive effects when Sedative-Hypnotics used in combination with these agents
CNS depressants
Common mechanism by which overdose result in death
Depression of medullary and cardiovascular centers
"Date rape drug" (3)
Flunitrazepam (rohypnol): a potent rapid onset benzo with marked amnestic properties

also chloral hydrate or gamma hydroxybutyrate
The most important sign of withdrawal syndrome
Excessive CNS stimulation (seizures)
Treatment of withdrawal syndrome involves
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
These agents are CNS depressants
Ethanol, Barbiturates, and Benzodiazepines
Withdrawal from this drug causes lethargy, irritability, and headache
W/D from this drug causes anxiety and mental discomfort
Treatments available for nicotine addiction
Patches, gum, nasal spray, psychotherapy, and bupropion
Chronic high dose abuse of nicotine leads to
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
Tolerance is marked and abstinence syndrome occurs
Amphetamine agents
Dextroamphetamines and methamphetamine

effects by binding to the monoamine transporters and increasing extracellular levels of the biogenic amines dopamine, norepinephrine and serotonin. It is hypothesized that d-amphetamine acts primarily on the dopaminergic systems, while l-amphetamine is comparatively norepinephrinergic. The primary reinforcing and behavioral-stimulant effects of amphetamine, however, are linked to enhanced dopaminergic activity, primarily in the mesolimbic DA system. Amphetamine binds to the dopamine transporter (DAT) and blocks the transporters ability to clear DA from the synaptic space. In addition, amphetamine is transported into the cell which leads to dopamine efflux (DA is transported out of the cell and into the synaptic space via reverse transport of the DAT
These agents are congeners of Amphetamine
DOM, STP, MDA, and MDMA "ecstasy"

Serotonin is a neurotransmitter believed to play a role in the regulation of mood and pleasure. MDMA causes serotonin vesicles in the neurons to release quantities of serotonin into the synapses. Although popular press accounts focus on the role of serotonin release, the mechanism by which MDMA causes its unusual psychoactivity is largely unknown. In vitro and nonhuman animal studies have established that MDMA also induces dopamine, norepinephrine, and acetylcholine release, and can act directly on a number of receptors, including a2-adrenergic (adrenaline) and 5HT2A(serotonin) receptors. MDMA promotes the release of several hormones including prolactin and the antidiuretic hormone vasopressin, which may be important in its occasional production of water intoxication or hyponatremia
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
Cocaine "super-speed"
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of this which is pathognomonic
PCP: phencyclidine or angel dust.

both horizontal and vertical nystagmus is pathognomonic

NMDA antagonist
Removal of PCP may be aided
Urinary acidification and activated charcoal or continual nasogastric suction
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
Cholinoreceptor-Activating & Cholinesterase-Inhibiting Drugs
Activating: Acetylcholine, carbachol, bethanechol, pilocarpine
Indirect: Neostigmine, pyridostigmine, physostigmine, edrophonium, echothiophate, parathion and malathion
Direct-Acting Cholinomimetic Agonists
Muscarinic agonists or parasympathomimetic
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
Only direct acting agent that is very lipid soluble and used in glaucoma
Pilocarpine also carbachol
These agents are used to treat dry mouth in Sjögren's syndrome
Cevimeline + pilocarpine
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
Carbamate with intermediate action postoperative and used for neurogenic ileus and urinary retention
Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
Treatment of myasthenia gravis
2 drugs used in the treatment of Alzheimers
Donepezil, tacrine
Antiglaucoma organophosphate
Associated with an increased incidence of cataracts in patients treated for glaucoma
Long acting cholinesterase inhibitors
Scabicide organophosphate
Organophosphate anthelmintic agent with long DOA
Toxicity of organophosphate:
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
The most important cause of acute deaths in cholinesterase inhibitor toxicity
Respiratory failure
The most toxic organophosphate
Treatment of choice for organophosphate overdose
Atropine and/or pralidoxime
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
Cholinoreceptor Blockers & Cholinesterase Regenerators
blockers: atropine, scopolamine, glycopyrrolate, ipratropium, tropicamide, oxybutynin, benztropine

Regenerator: Pralidoxime
Prototypical Nonselective Muscarinic Antagonists
Treat manifestations of Parkinson's disease and EPS
Benztropine, trihexyphenidyl
Treatment of motion sickness, may cause short term memory block
Antispasmodic, antisecretory, antiulcer, does not enter the CNS
Treatment of Antimuscarinic toxicity
Symptomatic + physostigmine(blocks acetylcholinesterase)
Name 6 other classes of drugs that have antimuscarinic effects as a SE
Antihistamine, Tricylic Antidepressants, Antipsychotics, Quinidine, Amantadine, Meperidine
Produce mydriasis and cycloplegia (4)
Atropine, homatropine, tropicamide, cyclopentolate
Bronchodilation in asthma and COPD
Reduce transient hyper GI motility (3)
Dicyclomine, methscopolamine, glycopyrrolate
Cystitis, postoperative bladder spasms, or incontinence (4)
Oxybutynin, dicyclomine, glycopyrrolate, tolterodine
Toxicity of anticholinergics
block SLUD (salivation, lacrimation, urination, defecation

dry as a bone, red as a beet, mad as a hatter
Another pneumonic for anticholinergic toxicity
"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
Atropine fever is the most dangerous effect and can be lethal in this population group
Contraindications to use of atropine
Infants, closed angle glaucoma, prostatic hypertrophy
Nicotinic Antagonists
Prototype ganglion blocker
Hexamethonium and Mecamylamine
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
Combined block of sympathetics and parasympathetics ex. postureal hypotension, dry mouth, blurred vision, constipation, sexual dysfunction
Main use for ganglionic blocker
Block ANS reflexes, allowing to see if change HR direct or autonomic
Will reverse the blockade by neuromuscular blockers
Cholinesterase inhibitors
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
Nondepolarizing Neuromuscular Blockers
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
Cholinesterase Regenerators
Used to treat patients exposed to insecticides such as parathion
1. epinephrine: general agonist
2. norepe: a1,a2,b1
3. phenylephrine, methoxamine, a1>a2
4. clonidine: a2>a1
5. isoproterenol: b1=b2
6. dobutamine b1>b2
7. terbutaline, albuterol: b2>b1
8. dopamine and bromocriptine: dop agonist
Which beta receptor does heart and which does lungs
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
Location of alpha 1 receptors (name at least 5)
Eye(myd), arterioles +veins = constrict, inhibits bladder, male sex organs, kidney(dec. renin), prostate(contract)
Location of alpha 2 receptors (name at least 3)
Prejunctional nerve terminals, aggregates platelets, pancreas(dec. insulin), fat cells to inhibit lipolysis
Location B1 receptors
nodes, heart muscle, kidney(inc. renin)
As increase dose of dopamine from low to high name receptor changes occuring
Low=D1, mid=also B1, high also a1
MAO of the liver
MAO of the brain
Locatoin B2 receptors (name at least 5)
all BV(dil), uterus, bronchioles, skeletal muscle get tremor, liver glycogenolysis, pancreas(inc. insulin)
This is the drug of choice for anaphylactic shock
Differ high dose epinephrine with norepinephrine
Alpha 1 blocker. See hypotension with epi.
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
At low dose epi is alpha or beta effect more prominent? High dose?
Low dose beta more responsive as more senstitive. High dose alpha due to being more numerous.
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
Epinephrine and dipivefrin are used for and MOA
Glaucoma: increase outflow via the uveoscleral veins
Newer alpha 2 agonist mechanism to treat glaucoma and name the two drugs