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800 Cards in this Set

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Half-life (T1/2)
Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
Volume of distribution (VD)
Relates the amount of drug in the body to the plasma concentration
Plasma concentration of a drug at a given time
Clearance (CL)
The ratio of the rate of elimination of a drug to its plasma concentration
First pass effect
The elimination of drug that occurs before it reaches the systemic circulation
Bioavailability (F)
The fraction of administered dose of a drug that reaches systemic circulation
Steady state
When the rate of drug input equals the rate of drug elimination
Phase I
This step of metabolism makes a drug more hydrophilic and hence augments elimination
Oxidation, reduction, hydrolysis
Different steps of Phase I
Barbiturates, phenytoin, carbamazepine, and rifampin
Inducers of Cytochrome P450 (CYP450)
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Inhibitors of CYP450
Glucuronate, acetic acid, and glutathione sulfate
Products of Phase II conjugation
First order kinetics
Type of kinetics when a constant percentage of substrate is metabolized per unit time
Zero order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Loading dose (Cp*(Vd/F))
Target plasma concentration times (volume of distribution divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Concentration in the plasma times (clearance divided by bioavailability)
Strength of interaction between drug and its receptor
Selectivity of a drug for its receptor
Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
Maximum response achieveable from a drug
Full agonist
Ability of a drug to produce 100% of the maximum response regardless of the potency
Partial agonist
Ability to produce less than 100% of the response
Competitive antagonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Noncompetitive antagonist
Class of drugs with ability to decrease the maximal response to an agonist
Thyroid and steroid hormones
A hormone whose mechanism of action (MOA) utilizes intracellular receptors
A hormone whose MOA utilizes transmembrane receptors
Benzodiazepines and calcium channel blockers
Class of drugs whose MOA utilizes ligand gated ion channels
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
Therapeutic index
Window between therapeutic effect and toxic effect
High therapeutic index
Term for a high margin of safety
Low therapeutic index
Term for a narrow margin of safety
Dimercaprol, EDTA
Antidote used for lead poisoning
Antidote used for cyanide poisoning
Antidote used for anticholinergic poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for organophosphate/anticholinesterase poisoning
Antidote used for iron salt toxicity
N-acetylcysteine (Mucomyst)
Antidote used for acetaminophen (APAP) toxicity
Antidote for arsenic, mercury, lead, and gold poisoning
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Antidote used for heparin overdose
Vitamin K and Fresh frozen plasma (FFP)
Antidote used for warfarin toxicity
Aminocaproic acid
Antidote for tissue plasminogen activator (t-PA), streptokinase
Ethanol or fomepizole
Antidote used for methanol and ethylene glycol
Naloxone (IV), naltrexone (PO)
Antidote used for opioid toxicity
Antidote used for benzodiazepine toxicity
Sodium bicarbonate
Antidote used for tricyclic antidepressants (TCA)
100% O2 and hyperbaric O2
Antidote used for carbon monoxide poisoning
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for digitalis toxicity
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Antidote for methotrexate toxicity
Antidote for beta-blockers and hypoglycemia
Magnesium sulfate
Antidote useful for some drug induced Torsade de pointes
sodium polystyrene sulfonate (Kayexalate)
Antidote for hyperkalemia
Alkalinize urine, dialysis
Antidote for salicylate intoxication
Log-kill hypothesis
Constant proportion of cell population killed rather than a constant number
Pulse therapy
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Rescue therapy
Toxic effect of anticancer drug can be lessened by rescue agents
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
5-flouracil (5-FU)
Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue
Drug used in cancer therapy causes Cushing-like symptoms
SEVERE myelosuppression
Side effect of Mitomycin
Alkylating agent
MOA of cisplatin
Nephro and ototoxicity
Common toxicities of cisplatin
6-mercaptopurine (6-MP)
Analog of hypoxanthine, needs HGPRTase for activation
Interaction with this drug requires dose reduction of 6-MP
May protect against doxorubicin toxicity by scavenging free radicals
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
Testicular cancer
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
Regimen used for non-Hodgkin's lymphoma
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Regimen used for breast cancer
Alkylating agent, vesicant that causes tissue damage with extravasation
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA)
Prevention of cyclophosphamide induced hemorrhagic cystitis
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Paclitaxel (taxol)
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
Interferon alpha
Used for hairy cell leukemia; it stimulates NK cells
Flutamide (Eulexin)
Anti-androgen used for prostate cancer
Anti-estrogen used for estrogen receptor + breast cancer
Letrozole, anastrozole
Aromatase inhibitor used in breast cancer
Toremifene (Fareston)
Newer estrogen receptor antagonist used in advanced breast cancer
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle specific anti-cancer drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
Some cell cycle non-specific drugs
Odansetron, granisetron
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonists
Carmustine (BCNU) and lomustine (CCNU)
Nitrosoureas with high lipophilicity, used for brain tumors
Produces disulfiram-like reaction with ethanol
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
GnRH antagonist with more immediate effects, used for infertility
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Hormone inhibiting prolactin release
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Desmopressin (DDAVP)
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Increased thromboembolic events
SE of OCs
L-thyroxine (T4)
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
T3 compound less widely used
Thioamides, iodides, radioactive iodine, and ipodate
Anti-thyroid drugs
Methimazole and propylthiouracil (PTU)
Thioamide agents used in hyperthyroidism
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
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
PTU (propylthiouracil) MOA
Iodide salts
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
Radioactive iodine
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radio contrast media that inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
Iron deiodinates thyroxine
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
Estogens increase maternal TBG
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
3 zones of adrenal cortex and their products
Pneumonic for 3 zones of adrenal cortex
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Cortisone and hydrocortisone (equivalent to cortisol)
Short acting glucocorticoids
Prednisone, methylprednisolone, prednisolone, and triamcinolone
Intermediate acting glucocorticoids
Betamethasone and dexamethasone
Long acting glucocorticoids
Fludrocortisone and deoxycorticosterone
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
Some side effects of corticosteroids
5-7 days
Period of time of therapy after which GC therapy will need to be tapered
Dexamethasone suppression test
Used for Cushing's syndrome (increased corticosteroid)
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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
Gynecomastia and hyperkalemia
Common SE of spironolactone
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Clomiphene and tamoxifen
Antiestrogen drugs used for fertility and breast cancer respectively
Hot flashes
Common SE of tamoxifen and raloxifene
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
Diethylstilbestrol (DES)
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
Ethinyl estradiol and mestranol
Estrogen mostly used in oral contraceptives (OC)
Mifepristone (RU-486)
Anti-progesterone used as abortifacient
Combination oral contraceptives (OC)
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
Oral contraceptive available in a transdermal patch
Converted to more active form DHT by 5 alpha-reductase
Finasteride (Proscar and Propecia respectively)
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
Nandrolone, oxymetholone, and oxandrolone
Anabolic steroid that has potential for abuse
Cyproterone acetate
Anti-androgen used for hirsutism in females
Drug is used with testosterone for male fertility
What do alpha cells in the pancreas produce?
What do beta cells in the pancreas produce?
Islets of Langerhans
Where are beta cells found in the pancreas?
What do delta cells in the pancreas produce?
Product of proinsulin cleavage used to assess insulin abuse
Little C-peptide
Exogenous insulin contains
Normal C-peptide
Endogenous insulin contains
Lispro (Humalog), aspart, glulisine
Very rapid acting insulin, having fastest onset and shortest duration of action
Regular (Humulin R)
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
Ultralente (humulin U)
Long acting insulin
Glargine (Lantus), detemir
Ultra long acting insulin, has over a day duration of action
Major SE of insulin
Important in synthesis of glucose to glycogen in the liver
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
Acarbose, miglitol
Examples of alpha-glucosidase inhibitors (AGI)
Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides
MOA of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
SE of AGI's
Alpha-glucosidase inhibitor associated with elevation of LFT's
Amino acid derivative, active as an insulin secretagogue
Insulin secretagogue - closes ATP-sensitive K+ channel
MOA of nateglinide
Glyburide, glipizide, and rosiglitazone
Drugs available in combination with metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
MOA of metformin
Decreased micro and macro vascular disease
Vascular effects of metformin
Lactic acidosis
Most important potential SE of metformin
Incidence of hyoglycemia with metformin
Meglitinide class of drugs
Insulin release from pancreas; faster and shorter acting than sulfonylurea
MOA of repaglinide
Chlorpropamide, tolbutamide, tolazamide, etc.
First generation sulfonylurea
Glyburide, glipizide, glimepiride, etc.
Second generation sulfonylurea
Insulin release from pancreas by modifying K+ channels
MOA of both generations
Common SE of sulfonylureas, repaglinide, and nateglinide
Sulfonylurea NOT recommended for elderly because of very long half life
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Hepatic toxicity
Reason troglitazone was withdrawn from market
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
MOA of thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
SE of Thiazolindinediones
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
Available bisphosphonates
Inhibits osteoclast bone resorption
MOA of Bisphosphonates
Pamidronate, zoledronate, ibandronate
Names of three bisphosphonates available IV
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Uses of bisphosphonates
Chemical esophagitis
Major SE of bisphosphonates
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Estrogen (HRT-Hormone replacement therapy)
Used for prevention of postmenopausal osteoporosis in women
Raloxifene (SERM-selective estrogen receptor modulator)
Increase bone density, also being tested for breast CA prophylaxis
Calcitonin (salmon prep)
Used intranasally and decreases bone resorption
Used especially in postmenopausal women, dosage should be 1500 mg
Vitamin D
Vitamin given with calcium to ensure proper absorption
St. Anthony's Fire
Disease caused by excess ergot alkaloids
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Zollinger-Ellison Syndrome
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Drug that causes contraction of the uterus
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
Distribution of histamine receptors H1, H2, and H3
Diphenhydramine and cimetridine, respectively
Prototype antagonist of H1 and H2 receptors
1st generation antihistamine that is highly sedating
Chlorpheniramine or cyclizine
1st generation antihistamine that is least sedating
Fexofenadine, loratadine, and cetirizine
2nd generation antihistamines
First generation due to being more lipid-soluble
Generation of antihistamine that has the most CNS effects
Use in IgE mediated allergic reaction
Major indication for H1 receptor antagonist
hydroxyzine (Atarax)
Antihistamine that can be used for anxiety and insomnia and is not addictive
Dimenhydrinate, meclizine, and other 1st generation
H1 antagonist used in motion sickness
Most common side effect of 1st generation antihistamines
Terfenadine and astemizole (have been removed from the market)
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
H2 blocker that causes the most interactions with other drugs
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Clinical use for H2 blockers
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
Receptors for serotonin (5HT-1) are located
Sumatriptan, naratriptan, and rizatriptan
"5HT-1d agonist used for migraine headaches "
Triptan available in parenteral and nasal formulation
H1 blocker that is also a serotonin antagonist
Oxytocin, ergonovine and ergotamine
Agents for reduction of postpartum bleeding
Ketanserin cyproheptadine, and phenoxybenzamine
Agents used in treatment of carcinoid tumor
Ondansetron, granisetron, dolasetron and alosetron
5HT-3 antagonist used in chemotherapeutic induced emesis
5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
DOC to treat chemo-induced nausea and vomiting
Drug used in ergot alkaloids overdose, ischemia and gangrene
Uterine contractions
Reason ergot alkaloids are contraindicated in pregnancy
Hallucinations resembling psychosis
SE of ergot alkaloids
Ergot alkaloid used as an illicit drug
Dopamine agonist used in hyperprolactinemia
Bradykinin and histamine
Peptide causing increased capillary permeability and edema
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)
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
Prostaglandins that cause abortions
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
Difference between COX 1 and COX 2
Celecoxib and rofecoxib
Drug that selectively inhibits COX 2
Inhibitor of lipoxygenase
Liver toxicity
Major SE of zileuton
Zafirlukast and montelukast
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Used in pediatrics to maintain patency of ductus arteriosis
PGI2 (epoprostenol)
Approved for use in severe pulmonary HTN
Prostaglandin used in the treatment of impotence
Irreversible, nonselective COX inhibitor
Class of drugs that reversibly inhibit COX
Primary endogenous substrate for Nitric Oxidase Synthase
Stimulates cGMP which leads to vascular smooth muscle relaxation
MOA and effect of nitric oxide
Long acting beta 2 agonist used in asthma
Muscarinic antagonist used in asthma
Mast cell stabilizer
MOA action of cromolyn
Methylxanthine derivative used as a remedy for intermittent claudication
inhibit phospholipase A2
MOA of corticosteroids
Adrenal suppression and weaning slowly, respectively
SE of long term (>5 days) corticosteroid therapy and remedy
Inhibit DNA gyrase
MOA of quinolones
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
MOA of penicillin
Drug used for MRSA
Blocks peptidoglycan synthesis
Vancomycin MOA
Point mutation
Type of resistance found with vancomycin
Meningitis prophylaxis in exposed patients
Scotch tape technique and mebendazole
Technique used to diagnose perianal itching, and the drug used to treat it
nephro and ototoxicity
Two toxicities of aminoglycosides
DOC for Legionnaires' disease
Inhibit dihydropteroate synthase
MOA of sulfonamides
Methicillin, nafcillin, and dicloxacillin
Penicillins active against penicillinase secreting bacteria
Cheap wide spectrum antibiotic DOC for otitis media
Class of antibiotics that have 10% cross sensitivity with penicillins
Carbenicillin, piperacillin and ticarcillin
PCN active against pseudomonas
Vancomycin, infusion at a slow rate and antihistamines
Antibiotic causing red-man syndrome, and prevention
Drug causes teeth discoloration
Decreases protein synthesis by inhibiting 30S ribosome
MOA of tetracycline
Drug that causes gray baby syndrome and aplastic anemia
Drug notorious for causing pseudomembranous colitis
DOC for tx of pseudomembranous colitis
ORAL vancomycin
Treatment of resistant pseudomembranous colitis
Megaloblastic anemia
Anemia caused by trimethoprim
Cartilage damage
Reason fluoroquinolones are contraindicated in children and pregnancy
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
Treatment for TB patients (think RIPE)
Disulfiram-like reaction
Metronidazole SE if given with alcohol
Red urine discoloration
Common side effect of Rifampin
Bind ergosterol in fungal cell membrane
MOA of nystatin
Administration of Vit. B6 (pyridoxine)
Neurotoxicity with isoniazid (INH) prevented by
Toxicity of amphotericin
SE seen only in men with administration of ketoconazole
Topical mupirocin (Bactroban)
Topical DOC in impetigo
DOC for influenza A
DOC for CMV retinitis
Neutro, leuko and thrombocytopenia
SE for ganciclovir
Nevirapine, amprenavir
Anti-viral agents associated with Stephen Johnson syndrome
Protease inhibitors
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Delavirdine, efavirenz, and ribavirin
Antivirals that are teratogens
Ganciclovir, zidovudine, saquinavir, and interferon
Antivirals associated with neutropenia
AZT (zidovudine)
HIV med used to reduce transmission during birth
Drug used for African sleeping sickness
Drug used in Chagas disease
Cefuroxime (2nd) generation, Ceftazidime, Ceftriaxone
Cephalosporins able to cross the BBB
Cefixime (3rd) generation
Cephalosporins NOT able to cross the BBB
Drug used for N. gonorrhea in females
Ceftriaxone or cefuroxime
Cephalosporin causes kernicterus in neonates
Peripheral neuritis and hepatitis
Aminoglycoside that is least ototoxic
Drug used in exoerythrocytic cycle of malaria
Oral antibiotic of choice for moderate inflammatory acne
Dapsone, rifampin and clofazimine combination
Drug of choice for leprosy
Acyclovir; incorporated into viral DNA and chain termination
DOC for herpes and its MOA
Anti-microbials that cause hemolysis in G6PD-deficient patients
Inhibition of protein synthesis at the 50s subunit of ribosome
MOA of erythromycin
sulfamethoxazole/ trimethoprim
Anti-biotic frequently used for chronic UTI prophylaxis
Lactam that can be used in PCN allergic patients
SE of imipenem
Anti-viral with a dose limiting toxicity of pancreatitis
Common side effect of hypnotic agents
Occurs when sedative hypnotics are used chronically or at high doses
Additive CNS depression
The most common type of drug interaction of sedative hypnotics with other depressant medications
Temazpam, trizolam, flurazepam
Benzodiazepines used to promote sleep
Benzodiazepine used for anxiety
Non-benzodiazepine used as an anxiolytic
Non-benzodiazepine used for sleep
REM is decreased
Major effect of benzodiazepines on sleep at high doses
Anterograde amnesia
Neurologic SE of benzodiazepines
Ability to cross the placenta
Reason benzos are used cautiously in pregnancy
Main route of metabolism for benzodiazepines
Lorazepam, oxazepam, and temazepam
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
increase the FREQUENCY of GABA-mediated chloride ion channel opening
MOA for benzodiazepines
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
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
Alprazolam and Clonazepam
Benzodiazepines that are the most effective in the treatment of panic disorder
Benzodiazepine that is used for anesthesia
DOC for status epilepticus
Chlordiazepoxide and Diazepam
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
Agents having active metabolites, long half lives, and a high incidence of adverse effects
Acute intermittent porphyria
Barbiturates may precipitate this hematologic condition
Liver enzyme INDUCTION
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Increase the DURATION of GABA-mediated chloride ion channels
Barbiturates MOA
Barbiturate used for the induction of anesthesia
Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
Site of action for zaleplon and zolpidem
Zolpidem, zaleplon
Good hypnotic activity with less CNS SE than most benzodiazepines
Agent that is a partial agonist for the 5-HT1A receptor
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Agent with zero-order kinetics
Aldehyde dehydrogenase
Rate limiting step of alcohol metabolism
System that increases in activity with chronic ethanol exposure and may contribute to tolerance
Aldehyde dehydrogenase
Enzyme that metabolizes acetaldehyde to acetate
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agents that inhibit acetaldehyde dehydrogenase
FOMEPIZOLE - used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
Agent that inhibits alcohol dyhydrogenase and its clinical use
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
The most common neurologic abnormality in chronic alcoholics
Agent that is teratogen and causes a fetal syndrome
Ethanol, fomepizole
Agent that is the antidote for methanol overdose
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Hepatic enzymes
Most frequent route of metabolism
Sodium channel blockade
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
GABA-related targets
MOA for benzodiazepines and barbiturates
Calcium channels
MOA for Ethosuximide
Affect calcium, potassium, and sodium channels
MOA for Valproic acid at high doses
Valproic acid and Phenytoin
Drugs of choice for generalized tonic-clonic and partial seizures
DOC for febrile seizures
Ethosuximide and valproic acid
Drugs of choice for absence seizures
Valproic acid
Drug of choice for myoclonic seizures
IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
Drugs of choice for status epilepticus
Drugs that can be used for infantile spasms
Valproic acid, carbamazepine, phenytoin and gabapentin
Anti-seizure drugs used also for bipolar affective disorder (BAD)
Anti-seizure drugs used also for Trigeminal neuralgia
Anti-seizure drugs used also for pain of neuropathic orgin
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
Gingival hyperplasia, nystagmus, diplopia and ataxia
SE of phenytoin
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
Valproic acid
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
Serum ammonia and LFT's
Laboratory value required to be monitored for patients on valproic acid
Stevens-Johnson syndrome
SE for Lamotrigine
Aplastic anemia and acute hepatic failure
SE for Felbamate
Valproic acid
Anti-seizure medication also used in the prevention of migraines
Carbamazepine may cause
Carbamazepine, gabapentin, lamotrigine, and valproic acid
Anti-seizure drugs used as alternative drugs for mood stabilization
Most are thought to act at GABA-A receptor - chloride channel
MOA of general anesthetics
Nitrous oxide
Inhaled anesthetic with a low blood/gas partition coefficient
Minimum alveolar anesthetic concentration (MAC)
Inversely related to potency of anesthetics
Halothane and methoxyflurane
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Decrease arterial blood pressure
Most inhaled anesthetics SE
Enflurane and halothane
Inhaled anesthetics are myocardial depressants
Inhaled anesthetic causes peripheral vasodilation
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Nitrous oxide
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Nitrous oxide
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
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
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
Block voltage-dependent sodium channels
MOA of local anesthetics (LA's)
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
Tetracaine and bupivacaine
Longer acting local anesthetics which are less dependent on vasoconstrictors
Cocaine and benzocaine
These LA's have surface activity
CNS toxicity
Most important toxic effects of most local anesthetics
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
LA causing methemoglobinemia
Neuromuscular blocking drugs
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
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
Nondepolarizing type antagonists
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)
Agent with long duration of action and is most likely to cause histamine release
Non-depolarizing skeletal muscle antagonist that has short duration
Skeletal muscle agent that can block muscarinic receptors
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
Cholinesterase inhibitors
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Spasmolytic drugs
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
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
Drug induced Parkinsonism
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
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, 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
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
Pramipexole and ropinirole
Non ergot agents used as first-line therapy in the initial management of Parkinson's
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 patients
Entacapone and Tolcapone
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
Agent effective in physiologic and essential tremor
Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
Agents used in Huntington's Disease
Haloperidol or pimozide
Agents used in Tourette's dx
Chelating agent used in Wilson's disease
Older antipsychotic agents, D2 receptors
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Dopamine blockade
MOA of neuroleptics
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
Side effects occuring in antipsychotics that block dopamine
Older antipsychotics
Antipsychotics that reduce positive symptoms only
Olanzapine, aripiprazole, and sertindole
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
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
Muscarinic blockers
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
Antipsychotic having the strongest autonomic effects
Antipsychotic having the weakest autonomic effects
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 fatal agranulocytosis
Anti-psychotic not shown to cause tardive dyskinesia
Fluphenazine and haloperidol
Anti-psychotics available in depot preparation
Low-potency typical antipsychotics and clozapine
Reduced seizure threshold
Low potency phenothiazines and ziprasidone
Orthostatic hypotension and QT prolongation
Increased risk of developing cataracts
Major route of elimination for Lithium
Lithium toxicity
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
Drug increases the renal clearance hence decreases levels of lithium
Cardiac anomalies and is contraindicated in pregnancy or lactation
Lithium is associated with this congenital defect
DOC for bipolar affective disorder
Low therapeutic index
Concern using lithium
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
SE of lithium
Clomipramine, fluoxetine and fluvoxamine
Example of three antidepressants that are indicated for obsessive compulsive disorder
Norepinephrine and serotonin
Neurotransmitters affected by the action of antidepressants
2 to 3 weeks
Usual time needed for full effect of antidepressant therapy
Elderly patients
Population group especially sensitive to side effects of antidepressants
Side-effect profile and prior pt response
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
SSRI's, bupropion, and venlafaxine
Well-tolerated and are first-line antidepressants
Monamine oxidase inhibitors
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
Hypertensive crisis
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
Serotonin syndrome
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
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
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
Three C's associated with TCA toxicity
Tertiary amines
Agents having higher sedation and antimuscarinic effects than other TCA's
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
Nortriptyline, Desipramine
Secondary amines that have less sedation and more excitation effect
Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
Side effects seen with tricyclic antidepressants
Antidepressant associated with neuroleptic malignant syndrome
Antidepressant associated with seizures and cardiotoxicity
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
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
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
Liver toxicity, increased serum cholesterol
SE of mirtazapine
Citalopram and its metabolite escitalopram
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
CNS stimulation; GI upset
Side effects frequently seen with SSRIs
Antidepressants with no effect on BP, no sedation
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
Fluoxetine (Sarafem)
SSRI indicated for premenstrual dysphoric disorder
Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
Some of SSRIs' therapeutic effects beside depression
SSRI less likely to cause a withdrawal syndrome
Ascending pathways
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
Presynaptic mu, delta, and kappa receptors
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
Postsynaptic Mu receptors
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
Miosis and constipation
Tolerance to all effects of opioid agonists can develop except
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
Opioid Analgesics
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
Morphine, methadone, meperidine, and fentanyl
Strong opioid agonists
Morphine and fentanyl
Opioids used in anesthesia
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
Codeine, hydrocodone, and oxycodone
Moderate opioid agonists
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
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
Dextromethorphan, Codeine
These agents are used as antitussive
Diphenoxylate, Loperamide
These agents are used as antidiarrheal
NO, chloroform, and diethyl ether
Inhalant anesthetics
Fluorocarbons and Industrial solvents
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
Organic nitrites
Cause dizziness, tachycardia, hypotension, and flushing
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
Heroin, morphine, oxycodone, meperidine and fentanyl
Most commonly abused in health care professionals
IV administration
This route is associated with rapid tolerance and psychologic dependence
Overdose of opioids
Leads to respiratory depression progressing to coma and death
Abstinence syndrome
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
Methadone, followed by slow dose reduction
Treatment for opioid addiction
This agent may cause more severe, rapid and intense symptoms to a recovering addict
Reduce inhibition, suppress anxiety, and produce relaxation
Sedative-Hypnotics action
CNS depressants
Additive effects when Sedative-Hypnotics used in combination with these agents
Depression of medullary and cardiovascular centers
Common mechanism by which overdose result in death
Flunitrazepam (rohypnol)
"Date rape drug"
Excessive CNS stimulation (seizures)
The most important sign of withdrawal syndrome
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
Treatment of withdrawal syndrome involves
Ethanol, Barbiturates, and Benzodiazepines
These agents are CNS depressants
Withdrawal from this drug causes lethargy, irritability, and headache
W/D from this drug causes anxiety and mental discomfort
Patches, gum, nasal spray, psychotherapy, and bupropion
Treatments available for nicotine addiction
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
Chronic high dose abuse of nicotine leads to
Tolerance is marked and abstinence syndrome occurs
Dextroamphetamines and methamphetamine
Amphetamine agents
DOM, STP, MDA, and MDMA "ecstasy"
These agents are congeners of Amphetamine
Cocaine "super-speed"
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic
Urinary acidification and activated charcoal or continual nasogastric suction
Removal of PCP may be aided
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
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
This agent used to treat dry mouth in Sjögren's syndrome
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
Carbamate with intermediate action, used for+A1170 postoperative and 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
Antiglaucoma organophosphate
Long acting cholinesterase inhibitors
Associated with an increased incidence of cataracts in patients treated for glaucoma
Scabicide organophosphate
Organophosphate anthelmintic agent with long DOA
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
Toxicity of organophosphate:
Respiratory failure
The most frequent cause of acute deaths in cholinesterase inhibitor toxicity
The most toxic organophosphate
Treatment of choice for organophosphate overdose
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
Nonselective Muscarinic Antagonists
Prototypical drug is atropine
Benztropine, trihexyphenidyl
Treat manifestations of Parkinson's disease and EPS
Scopolamine, meclizine
Treatment of motion sickness
Atropine, homatropine,C1208 tropicamide
Produce mydriasis and cycloplegia
Bronchodilation in asthma and COPD
Dicyclomine, methscopolamine
Reduce transient hyper GI motility
Oxybutynin, dicyclomine
Cystitis, postoperative bladder spasms, or incontinence
block SLUD (salivation, lacrimation, urination, defecation
Toxicity of anticholinergics
"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
Another pneumonic for anticholinergic toxicity
Atropine fever is the most dangerous effect and can be lethal in this population group
Infants, closed angle glaucoma, prostatic hypertrophy
Contraindications to use of atropine
Severe hypertension
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
Cholinesterase inhibitors
Reversal of blockade by neuromuscular blockers
Nondepolarizing Neuromuscular Blockers
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short duration of action
Cholinesterase regenerators, pralidoxime
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
Pralidoxime, atropine
Used to treat patients exposed to insecticides such as parathion
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
Pneumonic for beta receptors
This is the drug of choice for anaphylactic shock
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
Reduce aqueous secretion
Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma by acting to
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis
Longer acting Beta 2 agonist is recommended for prophylaxis of asthma
Beta1 agonists
These agents increase cardiac output and may be beneficial in treatment of acute heart failure and some types of shock
Alpha1 agonists
These agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
Increasing afterload and tissue perfusion declines
Shock due to septicemia or myocardial infarction is made worse by
Reduce the loss from area of injection
Epinephrine is often mixed with a local anesthetic to
Chronic orthostatic hypotension can be treated with
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses
Mast cells to reduce release of hisamine and inflammatory mediators
Agent used in shock because it dilates coronary arteries and increases renal blood flow
Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
Alpha 1 agonist toxicity
Sinus tachycardia and serious arrhythmias
Beta 1 agonist toxicity
Skeletal muscle tremor, tachycardia
Beta 2 agonist toxicity
high doses
The selective agents loose their selectivity at
Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis
Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena
Prazosin, terazosin, doxazosin
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
Selective Alpha-1A blocker, used for BPH, but with little effect on HTN
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
Acebutolol, atenolol, esmolol, metoprolol
SelectiveB1 Receptor blockers that may be useful in treating patients even though they have asthma
Labetalol and carvedilol
Combined alpha and beta blocking agents that may have application in treatment of CHF
Pindolol and acebutolol
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma
This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
This parenteral beta blocker is a short acting (minutes)
This beta blocker is the longest acting
Acebutolol and atenolol
These beta blockers are less lipid soluble
This beta blocker is highly lipid soluble and may account for side effects such as nightmares
Beta blockers
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, chronic CHF, and selected post MI patients
Beta blockers
Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF; signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)
Pilocarpine, carbachol, physostigmine
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
Epinephrine, dipivefrin
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
Apraclonidine, brimonidine
Selective alpha agonists that decreases aqueous secretion
Timolol (nonselective), betaxolol (selective)
These Beta blockers decrease aqueous secretion
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis
Prostaglandin PGF2a
This agent cause increased aqueous outflow
ACE inhibitors
Inhibit angiotensin-converting enzyme (ACE)
ACE inhibitors
Captopril and enalapril (-OPRIL ending) are
Dry cough, hyperkalemia
SE of ACE inhibitors
pregnancy and with K+
ACE inhibitors are contraindicated in
Angiotensin receptor
Losartan and valsartan block
Dry cough
Angiotensin receptor blockers do NOT cause
Calcium channel blockers
Agents that block L-type calcium channel
CCB contraindicated in CHF
CCB with predominate effect on arteriole dilation
Constipation, edema, and headache
Agents that reduce heart rate, contractility, and O2 demand
Beta-1 selective blockers
B-blockers that are more cardioselective
Atenolol, acebutolol, and metoprolol
Cardioselective Beta 1-blockers
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
Beta-blockers should be used cautiously in
Non-selective Beta-blocker also used for migraine prophylaxis
Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
SE of beta blockers
Prazosin, terazosin and doxazosin (-AZOSIN ending)
Alpha 1selective blockers
Non-selective Alpha1blockers use to treat pheochromocytoma
For rebound HTN from rapid clonidine withdrawal
Tamsulosin (Flomax)
A1a-selective blocker with no effects on HTN used for BPH
Orthostatic hypotension (especially with first dose) and reflex tachycardia
SE of alpha blockers
Clonidine, and methyldopa
Presynaptic Alpha 2 agonist used in HTN, and acts centrally
Positive Comb's test, depression
SE of methyldopa
Geriatrics due to its CNS (depression) effects
Methyldopa is contraindicated in
Rebound HTN, sedation, dry mouth
SE of clonidine
Direct vasodilator of arteriolar smooth muscle
Lupus-like syndrome
SE of hydralazine
Arterial vasodilator that works by opening K+ channels
SE of minoxidil
IV Drug used Hypertensive Crisis
Arteries and veins
Nitroprusside vasodilates
Cyanide toxicity treated with sodium thiosulfate
Toxicity caused by nitroprusside and treatment
Carbonic anhydrase inhibitor
Diuretic used for mountain sickness and glaucoma
Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
SE of acetazolamide
inhibits Na+/K+/2Cl- cotransport
MOA of loop diuretics
Thick ascending limb
Site of action of loop diuretics
Hyperuricemia, hypokalemia and ototoxicity
SE of loop (furosemide) diuretics
Aminoglycosides used with loop diuretics potentiate adverse effect
Loops lose and thiazide diuretics retain
Inhibit Na+/Cl- cotransport
MOA of thiazide diuretics
Work at early distal convoluted tubule
Site of action of thiazide diuretics
Class of drugs that may cause cross-sensitivity with thiazide diuretics
Hyperuricemia, hypokalemia and hyperglycemia
SE of thiazide (HCTZ) diuretics
Na+/K+ exchange
Potassium sparing diuretics inhibit
Diuretic used to treat primary aldosteronism
Gynecomastia hyperkalemia, and impotence
SE of spironolactone
Osmotic diuretic used to treat increased intracranial pressure
Desmopressin (DDAVP)
ADH agonist used for pituitary diabetes insipidus
Used for SIADH
Bone marrow and teeth discoloration for children under 8 years of age
SE of demeclocycline
Sodium channel blockers
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
Lupus-like syndrome
SE of procainamide
Prolongs QT interval
Limiting side effect of Quinidine
Thrombocytopenic purpura, and CINCHONISM
Other side effects of Quinidine
Increases concentration of Digoxin
Major drug interaction with Quinidine
DOC for management of acute ventricular arrhythmias
DOC for digoxin induced arrhythmias
Gingival hyperplasia
SE of phenytoin
Class IC (flecainide, propafenone, moricizine)
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
Class II antiarrhythmics are
Antiarrhythmic that exhibits Class II and III properties
prolongs QT and PR interval
Side effect of sotalol
Used intravenously for acute arrhythmias during surgery
Anti-arrhythmics that decrease mortality
Potassium channel blockers
MOA of class III antiarrhythmics
Class III antiarrhythmic that exhibits properties of all 4 classes
Prolonged half-life, up to six weeks
Specific pharmacokinetic characteristic of amiodarone
Antiarrhythmic effective in most types of arrhythmia
Cardiac dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits
SE of Amiodarone
Calcium channel blockers
MOA of class IV antiarrhythmics
Torsades de pointes
Life threatening cardiac event that prolong QT leads to
Magnesium sulfate
Agent to treat torsades de pointes
Drug used supraventricular arrhythmias
DOC for paroxysmal supraventricular tachycardia (PSVT)
Activattion on an inward K+ current and inhibition of Ca++ current resulting in marked hyperpolarization
Adenosine's MOA
Anti-arrhythmic with 15 second duration of action
Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
MOA of sildenafil (Viagra)
Aspirin, Nitrates, CCB, and Beta blockers
Drugs used in the management of angina
Platelet aggregation inhibition
Aspirin reduces mortality in unstable angina by
Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
MOA of nitrates
Nitroglycerin sublingual tablets
Nitrate used for acute anginal attacks
Oral and transdermal forms of nitroglycerin
Nitrate used to prevent further attacks
Nitrate free intervals are needed due to
Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation
SE of nitrates
Prinzmetal's angina
CCB are DOC for
Beta blockers are used for which type of anginal attack
Indirectly increase intracellular calcium and cardiac contractility by inhibiting Na+/K+ ATPase
MOA of Cardiac glycosides (eg. digoxin)
Atrial fibrillation and CHF
Digoxin is used in
Digoxin toxicity can be precipitated by
Antidote for digoxin toxicity
Amrinone and milrinone
Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects
SE of amrinone
Dobutamine and dopamine
Beta 1 agonists used in acute CHF
Reducing preload
Diuretics work in CHF by
Reducing progression of heart failure (never use in acute heart failure)
Beta blockers work in CHF by
Nesiritide (BNP)
Peptide drug used to treat CHF
Increasing sodium excretion and decreases arterial and venous tone
MOA of nesiritide
Excessive hypotension and kidney failure
SE of nesiritide
Agent used in CHF that is a selective alpha and nonselective beta blocker
Nesiritide (Natrecor)
Agent used in acutely decompensated CHF resembling natriuretic peptide
Warfarin (PT)
Vitamin K dependent anticoagulant
Warfarin is contraindicated in
Anticoagulant of choice in pregnancy
Antithrombin 3
Heparin (PTT) increases activity of
Route of administration of warfarin
IV and IM (only LMW)
Routes of administration of heparin
SE of both warfarin and heparin
Heparin induced thrombocytopenia (HIT)
SE of heparin
Alternative anticoagulant used if HIT develops
Vitamin K or fresh frozen plasma
Antidote to reverse actions of warfarin
Protamine sulfate
Antidote to reverse actions of heparin
Irreversibly blocking cyclooxygenase
MOA of aspirin
Aspirin, metoprolol
Agent used to treat MI and to reduce incidence of subsequent MI
GI bleeding
SE of Aspirin
Antiplatelet drug reserved for patients allergic to aspirin
Neutropenia and agranulocytosis
SE for ticlopidine
Clopidogrel and ticlopidine
Effective in preventing TIA's
Prevents thrombosis in patients with artificial heart valve
Abciximab, tirofiban and eptifibatide
Block glycoprotein IIb/IIIa involved in platelet cross-linking
Degradation of fibrin clots and are administered IV
MOA of thrombolytics
Pulmonary embolism and DVT
Thrombolytics are used for
Thrombolytic that can cause allergic reaction
Tissue plasmin activator
Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA
Cerebral hemorrhage
SE of tPA
Aminocaproic acid
Antidote for thrombolytics
Ferrous sulfate
Agent to treat hypochromic microcytic anemias
Chelating agent used in acute iron toxicity
Cyanocobalamin (Vit B12)
Agent for pernicious anemia
Vitamin B12
Agent used for neurological deficits in megaloblastic anemia
Folic acid
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
Agent used for anemias associated with renal failure
G-CSF (filgrastim) and GM-CSF (sargramostim)
Agent used neutropenia especially after chemotherapy
Interleukin 11 (oprelvekin)
Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy
Bile acid-binding resins
Drugs decrease intestinal absorption of cholesterol
Bile acid-binding resins
Cholestyramine and colestipol are
Impair absorption of fat soluble vitamin absorption (A,D,E,K)
Major nutritional side effect of bile acid-binding resins
inhibits HMG COA reductase
MOA of lovastatin (STATIN)
HMG CoA reductase inhibitors are contraindicated in
Inhibit Cytochrome P450 3A4
MOA of drug or foods (grapefruit juice) that increase statin effect
Rhabdomyolysis and Hepatotoxicity
SE of HMG COA reductase inhibitors
Monitoring parameter to obtain before initiation of STATINS
Decreases liver triglycerol synthesis
Cutaneous flush
SE of niacin
Cutaneous flush and be reduced by pretreatment with
Lipoprotein lipase
Fibrates (gemfibrozil) increase activity of
Most common SE of fibrates
Fibrates are contraindicated in
Concurrent use of fibrates and statins increases risk of
Ezetimibe (Zetia)
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)
Aspirin irreversibly inhibits cyclooxygenase
Difference between aspirin and other NSAIDS
Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
Four main actions of NSAIDS
Agent used for closure of patent ductus arteriosus
Potential for development of Reye's syndrome
Aspirin is contraindicated in children with viral infection
Tinnitus, GI bleeding
SE of salicylates
Diclofenac, ketoralac
NSAID also available as an ophthalmic preparation
NSAID available orally, IM and ophthalmically
NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity
Newer NSAID that selectively inhibits COX-2
Gastric ulcers and GI Bleeding
COX 2 inhibitors may have reduced risk of
Pre-existing cardiac or renal disease
COX 2 inhibitors should be used cautiously in pts with
Antipyretic and analgesic activity
Acetaminophen only has
SE of acetaminophen
Antidote for acetaminophen toxicity
Rheumatic disease
DMARDs are slow acting drugs for
Initial DMARD of choice for patients with RA
Drug ofter used in combination with TNF - alpha inhitors for RA
Causes bone marrow suppression
Aplastic anemia and renal toxicity
SE of penicillamine
Interferes with activity of T-lymphocytes
Anti-malarial drug used in rheumatoid arthritis (RA)
Retinal destruction and dermatitis
SE of hydroxychloroquine
Inhibiting dihydroorotate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T cell proliferation and decreased antibody production by B cells
MOA of Leflunomide (newer agent)
Adalimumab, infliximab and etanercept
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha)
Anti-rheumatic agent also used for ulcerative colitis
Anti-rheumatic agent also used for Chron's disease
NSAID used in gout
NSAID contraindicated in gout
Selective inhibitor of microtubule assembly
MOA of colchicine (used in acute gout)
Kidney and liver toxicity, diarrhea
SE of colchicine
Probenecid and sulfinpyrazone
Agent used to treat chronic gout by increasing uric acid secretion and excretion
Xanthine oxidase
Allopurinol treats chronic gout by decreasing uric acid production by inhibiting
lispro insulin, aspart insulin, glulisine insulin
Rapid acting insulins that do not self-aggregate
Insulin glargine
Peakless ling acting insulin
DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action