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796 Cards in this Set

  • Front
  • Back
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)
Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
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 the systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
This step of metabolism makes a 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, rifampin, St. John's Wort
Inhibitors of CYP450
Amiodarone, Diltiazem, Verapamil, Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
Type of kinetics when a constant percentage of substrate is metabolized per unit time
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
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
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full agonist
Ability to 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
Class of drugs with ability to decrease the maximal response to an agonist
Noncompetitive antagonist
A hormone whose mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
A hormone whose MOA utilizes transmembrane receptors
Class of drugs whose MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
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
Therapeutic index
Term for a high margin of safety
High therapeutic index
Term for a narrow margin of safety
Low therapeutic index
Antidote used for lead poisoning
Dimercaprol, EDTA
Antidote used for cyanide poisoning
Antidote used for anticholinergic poisoning
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst)
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
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Ethanol or fomepizole
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digibind (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
Antidote for beta-blockers and hypoglycemia
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate(Kayexalate)
Antidote for salicylate intoxication
Alkalinize urine, dialysis
Relationship of tumor cell number to time of diagnosis, symptoms, treatment and survival
Log-kill hypothesis
Pyrimidine analog that causes "thymineless death" given with leucovorin rescue
5-fluorouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Side effect of Mitomycin
SEVERE myelosuppression
MOA of cisplatin
Alkylating agent
Common toxicities of cisplatin
Nephro and ototoxicity, peripheral neuropathy
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6- MP
Iron-chelating agent, protects against doxorubicin toxicity by scavenging free radicals
Blows DNA (breaks DNA strands), limiting SE is pulmonary toxicity
Platinum-based combination therapy for testicular cancer
ABVD regimen used for Hodgkin's, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin,,vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphoma
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Microtubule inhibitor that causes peripheral sensory neuropathy , foot drop (eg. ataxia), and SIADH
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxel (taxol)
Agent similar to cisplatin, less nephrotoxic, greater myelosuppression, used to treat refractory hematologic malignancies
Anti-androgen used for prostate cancer
Flutamide, bicalutamide, nilutamide
Anti-estrogen used for estrogen receptor + breast cancer
Aromatase inhibitor used in breast cancer
Newer biologic agent approved for metastatic melanoma, enhances T-cell immune responses
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
Regimen used for advanced colorectal cancer, stageII and III colon cancer
FOLFOX (oxaliplatin, 5-FU and leucovorin)
Nitrosoureas with high lipophilicity, used for brain tumors
Anti-cancer agents that affect the VEGF-signaling pathway
Bevacizumab, Ziv-aflibercept, Sorafenib, Sunitinib, Pazopanib
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
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
SE of OCs
Increased thromboembolic events
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
T3 compound less widely used
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
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts
Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
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
Beta-blockers such as propranolol
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
Iron deiodinates thyroxine
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
Estogens increase maternal TBG
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Mnemonic for 3 zones of adrenal cortex
Used for Addison's disease , Congenital Adrenal Hyperplasia (CAH) , inflammation, allergies, and asthma (as a local inhalation)
Short-medium acting glucocorticoids
Cortisone, Hydrocortisone, Prednisone, Prednisolone, Methylprednisolone
Intermediate acting glucocorticoids
Triamcinolone, Fluprednisolone
Long acting glucocorticoids
Betamethasone and dexamethasone
Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
Used for Cushing's syndrome (increased corticosteroid)
Dexamethasone suppression test
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
Common SE of spironolactone
Gynecomastia and hyperkalemia
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Antiestrogen drugs used for fertility and breast cancer respectively
Clomiphene and tamoxifen
Common SE of tamoxifen and raloxifene
Hot flashes
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
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)
Ethinyl estradiol and mestranol
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 by 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, oxymetholone, and oxandrolone
Anti-androgen used for hirsutism in females
Cyproterone acetate
Drug is used with testosterone for male fertility
What do alpha cells in the pancreas produce?
What do beta cells in the pancreas produce?
Where are beta cells found in the pancreas?
Islets of Langerhans
What do delta cells in the pancreas produce?
Product of proinsulin cleavage used to assess insulin production
Exogenous insulin contains
No C-peptide
Endogenous insulin contains
Normal C-peptide
Very rapid acting insulin, having fastest onset and
Lispro (Humalog), aspart (Novolog),
shortest duration of action
glulisine (Apidra)
Short acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin/Novolin R)
Long acting insulins
Glargine, detemir
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
Examples of alpha-glucosidase inhibitors (AGI)
Acarbose, miglitol
MOA of AGI's
Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides
SE of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's
Amino acid derivative, active as an insulin secretagogue
MOA of nateglinide
Insulin secretagogue - closes ATP- sensitive K+ channel
Drugs available in combination with metformin
Glyburide, glipizide, sitagliptin, saxagliptin, pioglitazone
MOA of metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
Vascular effects of metformin
Decreased micro and macro vascular disease
Most important potential SE of metformin
Lactic acidosis
Incidence of hyoglycemia with metformin
Meglitinide class of drugs
MOA of repaglinide
Insulin release from pancreas; faster and shorter acting than sulfonylurea
First generation sulfonylurea
Chlorpropamide, tolbutamide, tolazamide, etc.
Second generation sulfonylurea
Glyburide, glipizide, glimepiride, etc.
MOA of both generations
Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide
Hypoglycemia, weight gain
Sulfonylurea NOT recommended for elderly because of very long half life
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Reason troglitazone was withdrawn from market
Hepatic toxicity
MOA of thiazolidinediones
Decrease insulin resistance, stimulate PPAR-gamma receptors
SE of Thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism, risk for angina/MI
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta- blocker overdose and smooth muscle relaxation
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Names of three bisphosphonates available IV
Pamidronate, zoledronate, ibandronate
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Major SE of bisphosphonates
Chemical esophagitis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CA prophlaxis
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
Disease caused by excess ergot alkaloids
St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
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
Diphenhydramine and cimetidine, respectively
1st generation antihistamine that is highly sedating
1st generation antihistamine that is least sedating
Chlorpheniramine or cyclizine
2nd generation antihistamines
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 antagonist used in motion sickness
Dimenhydrinate, meclizine, and other 1st generation
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 (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
5HT-1d agonist used for migraine headaches
Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation
H1 blocker that is also a serotonin antagonist
Agents for reduction of postpartum bleeding
Oxytocin, ergonovine and ergotamine
Agents used in treatment of carcinoid tumor
Ketanserin cyproheptadine, and phenoxybenzamine
5HT-3 antagonist used in chemotherapeutic induced emesis
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
DOC to treat chemo-induced nausea and vomiting
Drug used in ergot alkaloids overdose, ischemia and gangrene
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE of ergot alkaloids
Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug
Dopamine agonist used in hyperprolactinemia
Peptide causing increased capillary permeability and edema
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
Drug that selectively inhibits COX 2
Celecoxib and rofecoxib
Inhibitor of lipoxygenase
Major SE of zileuton
Liver toxicity
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Zafirlukast and montelukast
Used in pediatrics to maintain patency of ductus arteriosis
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
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
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
Long acting beta 2 agonist used in asthma
Salmeterol, formoterol
Muscarinic antagonist used in asthma
MOA action of cromolyn
Mast cell stabilizer
Methylxanthine derivative used as a remedy for intermittent claudication
MOA of corticosteroids
inhibit phospholipase A2
SE of long term corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
MOA of quinolones
Inhibit DNA gyrase
MOA of penicillin
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
Drug used for MRSA
Vancomycin MOA
Blocks cell wall synthesis by sequestration
Genetic basis of low level resistance found with vancomycin
Point mutation
Meningitis prophylaxis for persons in contact with patients
Ciprofloxacin or Rifampin (for children less than 4 yrs old)
Technique used to diagnose perianal itching, and the drug used to treat it
Scotch tape technique and mebendazole
Two toxicities of aminoglycosides
nephro and ototoxicity
DOC for Legionnaires' disease
MOA of sulfonamides
Inhibit dihydropteroate synthase
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC for otitis media
Class of antibiotics that have 10% cross sensitivity with penicillins
PCN active against pseudomonas
ceftazidime, imipenem, 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
Drug notorious for causing pseudomembranous colitis
Clindamycin, metronidazole
DOC for tx of pseudomembranous colitis (mild)
Treatment of severe/relapsing pseudomembranous colitis
ORAL vancomycin
Anemia caused by trimethoprim
Megaloblastic anemia
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
DOC for giardia, bacterial vaginosis, and trichomonas
Treatment for TB patients (think RIPE)
R ifampin, I soniazid, P yrazinamide, and E thambutol
Metronidazole SE if given with alcohol
Disulfiram-like reaction
Common side effect of Rifampin
Red urine discoloration
MOA of nystatin
Bind ergosterol in fungal cell membrane
Neurotoxicity with isoniazid (INH) prevented by
Administration of Vit. B6 (pyridoxine)
Toxicity of amphotericin
SE seen only in men with administration of ketoconazole
Topical DOC in impetigo
Topical mupirocin (Bactroban)
Drug used for African sleeping sickness
Drug used in Chagas disease
Cephalosporins able to cross the BBB
Ceftazidime, Ceftriaxone or Cefotaxime
Oral 3rd generation cephalosporins NOT able to cross the BBB
Drug used for N. gonorrhea in females
Cephalosporin causes kernicterus in neonates
Ceftriaxone or cefuroxime
Peripheral neuritis and hepatitis
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
Dapsone, rifampin and clofazimine combination
DOC for herpes and its MOA
Acyclovir; phosphorylation, incorporation into viral DNA, and chain termination
Anti-bacterials 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
sulfamethoxazole/ trimethoprim
Lactams that can be used in PCN allergic patients
SE of imipenem
DOC for influenza A
DOC for severe RSV
DOC for CMV retinitis
Ganciclovir, valganciclovir
SE for ganciclovir
Anti-viral agent associated with Stephen Johnson syndrome
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Protease inhibitors
Protease inhibitors recommended for pregnant women
lopinavir, ritonavir, atazanavir
Antivirals that are teratogens
Delavirdine, efavirenz, and ribavirin
Single dose used to prevent perinatal transmission of HIV
Anti-viral with a dose limiting toxicity of pancreatitis
Anti-HSV/VZV agent that causes thrombotic thrombocytopenic purpura/hemolytic uremic syndrome in high doses
Intravenous drug effective for end-organ CMV disease (retinitis, colitis, esophagitis)
Nucleoside reverse transcriptase inhibitor that can cause fatal hypersensitivity reactions linked to HLDB5701
Polymerase inhibitor used to treat Hepatitis C infections in combination with ribavarin
Protease inhibitors used to treat Hepatitis C infections
Boceprevir, Simeprevir, Telaprevir
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
Benzodiazepines used to promote sleep
Temazpam, trizolam, flurazepam
Benzodiazepine used for anxiety
Non-benzodiazepine used as an anxiolytic
Non-benzodiazepine used for sleep
Major effect of benzodiazepines on sleep at high doses
REM is decreased
Neurologic SE of benzodiazepines
Anterograde amnesia
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
Main route of metabolism for benzodiazepines
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
MOA for benzodiazepines
increase the FREQUENCY of GABA- mediated chloride ion channel opening
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
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
Benzodiazepine that is used for anesthesia
DOC for status epilepticus
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
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
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
Increase the DURATION of GABA- mediated chloride ion channels
Barbiturate used for the induction of anesthesia
Site of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
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
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
System that increases in activity with chronic ethanol exposure and may contribute to tolerance
Enzyme that metabolizes acetaldehyde to acetate
Aldehyde dehydrogenase
Agents that inhibit acetaldehyde dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agent that inhibits alcohol dyhydrogenase and its clinical use
FOMEPIZOLE - used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
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
Ethanol, fomepizole
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Most frequent route of metabolism
Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
Sodium channel blockade
MOA for benzodiazepines and barbiturates
GABA-related targets
MOA for Ethosuximide
Calcium channels
MOA for Valproic acid at high doses
Affect calcium, potassium, and sodium channels
Drugs of choice for generalized tonic-clonic and partial seizures
Valproic acid and Phenytoin
DOC for febrile seizures
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 for short term (acute) treatment; phenytoin for prolonged therapy
Drugs that can be used for infantile spasms
Anti-seizure drugs used also for bipolar affective disorder (BAD)
Valproic acid, carbamazepine, phenytoin and gabapentin
Anti-seizure drugs used also for Trigeminal neuralgia
Anti-seizure drugs used also for pain of neuropathic origin
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
Valproic acid
Carbamazepine may cause
Anti-seizure drugs used as alternative drugs for mood stabilization
Carbamazepine, gabapentin, lamotrigine, and valproic acid
MOA of general anesthetics
Most are thought to act at GABA-A receptor - chloride channel
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC)
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
H alothane
Inhaled anesthetic, 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
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
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
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
Inhaled anesthetics, especially isoflurane,
neuromuscular blockade (NMB)
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 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
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Cholinesterase inhibitors
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
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
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
Drug induced Parkinsonism
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
Non ergot 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 slows down metabolism of dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
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
Agents used in Huntington's Disease
Tetrabenazine (amine depleting drug), reserpine
Agents used in Tourette's dx
Haloperidol, pimozide , clonidine
Chelating agent used in Wilson's disease
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Older antipsychotic agents, D2 receptors
MOA of neuroleptics
Dopamine blockade
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
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
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
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 phenothiazines and ziprasidone
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
Concern using lithium
Low therapeutic index
SE of lithium
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
Example of three antidepressants that are indicated
Clomipramine, fluoxetine and
for obsessive compulsive disorder
Neurotransmitters affected by the action of antidepressants
Norepinephrine and serotonin
Usual time needed for full effect of antidepressant therapy
2 to 6 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, drug interaction potential and prior pt response
Well-tolerated and are first-line antidepressants Monoamine oxidase inhibitors (MAOI)
SSRI's, bupropion, and venlafaxine
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 Tricyclic antidepressants (TCA)
Serotonin syndrome
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
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
Side effects seen with tricyclic antidepressants
Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
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
Venlafaxine, duloxetine
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
SE of mirtazapine
Liver toxicity, increased serum cholesterol
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
Citalopram and its metabolite escitalopram
Side effects frequently seen with SSRIs
CNS stimulation; GI upset
Antidepressants with no effect on BP, no sedation
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
Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
SSRI less likely to cause a withdrawal syndrome
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
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
Opioid Analgesics
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 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
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
Cause dizziness, tachycardia, hypotension, and flushing
Organic nitrites
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
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
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
Abstinence 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"
Flunitrazepam (rohypnol)
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
These agents are congeners of Amphetamine
DOM, STP, MDA, and MDMA "ecstasy"
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 both horizontal and vertical nystagmus is pathognomonic
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
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 Organophosphates
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 frequent cause of acute deaths in cholinesterase inhibitor toxicity
Respiratory failure
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
Prototypical drug is atropine
Nonselective Muscarinic Antagonists
Treat manifestations of Parkinson's disease and EPS
Benztropine, trihexyphenidyl
Treatment of motion sickness
Scopolamine, meclizine
Produce mydriasis and cycloplegia
Atropine, homatropine,C1208 tropicamide
Bronchodilation in asthma and COPD
Reduce transient hyper GI motility
Dicyclomine, methscopolamine
Cystitis, postoperative bladder spasms, or incontinence
Oxybutynin, dicyclomine
Toxicity of anticholinergics
block SLUD (salivation, lacrimation, urination, defecation)
Another mnemonic 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
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
Severe hypertension
Reversal of 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; has short duration of action
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
Cholinesterase regenerators, pralidoxime
Used to treat patients exposed to insecticides such as parathion
Pralidoxime, atropine
Mnemonic for beta receptors
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
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
Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma by acting to
Reduce aqueous secretion
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
Salmeterol, formoterol (both in combination with corticosteroid; contraindicated as monotherapy)
These agents increase cardiac output and may be beneficial in treatment of acute heart failure and some types of shock
Beta1 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
Alpha1 agonists
Shock due to septicemia or myocardial infarction is made worse by
Increasing afterload and tissue perfusion declines
Epinephrine is often mixed with a local anesthetic to
Reduce the loss from area of injection
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
Beta 1 agonist toxicity
Sinus tachycardia and serious arrhythmias
Beta 2 agonist toxicity
Skeletal muscle tremor, tachycardia
The selective agents loose their selectivity at
high doses
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
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
Prazosin, terazosin, doxazosin
Selective Alpha-1A blocker, used for BPH, but with little effect on HTN
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
SelectiveB1 Receptor blockers that may be useful in treating patients even though they have asthma
Acebutolol, atenolol, esmolol, metoprolol
Combined alpha and beta blocking agents that may have application in treatment of CHF
Labetalol and carvedilol
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma
Pindolol and acebutolol
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
These beta blockers are less lipid soluble
Acebutolol and atenolol
This beta blocker is highly lipid soluble and may account for side effects such as nightmares
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)
Beta blockers
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
Pilocarpine, carbachol, physostigmine
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
Epinephrine, dipivefrin
Selective alpha agonists that decreases aqueous secretion
Apraclonidine, brimonidine
These Beta blockers decrease aqueous secretion
Timolol (nonselective), betaxolol (selective)
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
This agent cause increased aqueous outflow
Prostaglandin PGF2a
Inhibit peptidyl dipeptidase (plasma kininase)
ACE inhibitors
SE of ACE inhibitors
Cough, hyperkalemia, angioedema
ACE inhibitors are contraindicated in
pregnancy and with K+
Losartan and valsartan block
Angiotensin AT1 receptor
Angiotensin receptor blockers do NOT effect
Bradykinin metabolism
Agents that block L-type calcium channel
Calcium channel blockers
CCB contraindicated in CHF
CCB with predominant effect on vasodilation
atrioventricular block, constipation, edema
Agents that reduce heart rate, contractility, and O2 demand
B-blockers that are more cardioselective
Beta-1 selective blockers (AMEBBA - atenolol, metoprolol, esmolol, betaxolol, bisoprolol, acebutalol)
Beta-blockers should be used cautiously in
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
Non-selective Beta-blocker also used for migraine prophylaxis
SE of beta blockers
Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
Alpha 1selective blockers
Prazosin, terazosin and doxazosin (- AZOSIN ending)
Non-selective Alpha1blockers use to treat pheochromocytoma
For rebound HTN from rapid clonidine withdrawal
SE of alpha blockers
Orthostatic hypotension (especially with first dose) and reflex tachycardia
Partial Alpha agonist used in HTN, acts centrally
Used primarily for hypertension during pregnancy, can give positive Coomb's test
SE of clonidine
sedation, dry mouth, mental depression
Direct vasodilator of arteriolar smooth muscle
SE of hydralazine with slow acetylators
Lupus-like syndrome
Arterial vasodilator that works by opening K+ channels
SE of minoxidil
IV Drug used Hypertensive Crisis
Nitroprusside, fenoldopam, labetalol
Nitroprusside vasodilates
Arteries and veins
Toxicity caused by nitroprusside and treatment
Cyanide toxicity treated with sodium thiosulfate
Carbonic anhydrase inhibitor
Diuretic used for mountain sickness and glaucoma
SE of acetazolamide
Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
MOA of loop diuretics
inhibits Na+/K+/2Cl- cotransport
Site of action of loop diuretics
Thick ascending limb
SE of loop (furosemide) diuretics
Hyperuricemia, hypokalemia and ototoxicity
Aminoglycosides used with loop diuretics potentiate adverse effect
Loops lose and thiazide diuretics retain
MOA of thiazide diuretics
Inhibit Na+/Cl- cotransport
Site of action of thiazide diuretics
Work at early distal convoluted tubule
Class of drugs that may cause cross-sensitivity with thiazide diuretics
SE of thiazide (HCTZ) diuretics
Hyperuricemia, hypokalemia and hyperglycemia
Potassium sparing diuretics inhibit
Na+/K+ exchange
Diuretic used to treat primary aldosteronism
SE of spironolactone
Gynecomastia, hyperkalemia
Osmotic diuretic used to treat increased intracranial pressure
ADH agonist used for pituitary diabetes insipidus
Desmopressin (DDAVP)
Used for SIADH
SE of demeclocycline
Bone marrow and teeth discoloration for children under 8 years of age
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
Sodium channel blockers
SE of procainamide
Lupus-like syndrome
Limiting side effect of Quinidine
Prolongs QT interval
Other side effects of Quinidine
Thrombocytopenic purpura, and CINCHONISM
Major drug interaction with Quinidine
Increases concentration of Digoxin
DOC for management of acute ventricular arrhythmias
DOC for digoxin induced arrhythmias
SE of phenytoin
Gingival hyperplasia
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
Class IC (flecainide, propafenone, moricizine)
Class II antiarrhythmics are
Antiarrhythmic that exhibits Class II and III properties
Side effect of sotalol
prolongs QT and PR interval
Used intravenously for acute arrhythmias during surgery
Anti-arrhythmics that decrease mortality
MOA of class III antiarrhythmics
Potassium channel blockers
Class III antiarrhythmic that exhibits properties of all 4 classes
Specific pharmacokinetic characteristic of amiodarone
Prolonged half-life, up to six weeks
Antiarrhythmic effective in most types of arrhythmia
SE of Amiodarone
Cardiac dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits
MOA of class IV antiarrhythmics
Calcium channel blockers
Life threatening cardiac event that prolong QT to
Torsades de pointes
Agent to treat torsades de pointes
Magnesium sulfate
Drug used supraventricular arrhythmias
DOC for paroxysmal supraventricular tachycardia (PSVT)
Adenosine's MOA
Activattion on an inward K+ current and inhibition of Ca++ current resulting in marked hyperpolarization
Anti-arrhythmic with 15 second duration of action
MOA of sildenafil (Viagra)
Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
Drugs used in the management of angina
Aspirin, Nitrates, CCB, and Beta blockers
Aspirin reduces mortality in unstable angina by
Platelet aggregation inhibition
MOA of nitrates
Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
Nitrate used for acute anginal attacks
Nitroglycerin sublingual tablets
Nitrate used to prevent further attacks
Oral and transdermal forms of nitroglycerin
Nitrate free intervals are needed due to
SE of nitrates
Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation
CCB are DOC for
Prinzmetal's angina
Beta blockers are used for which type of anginal attack
MOA of Cardiac glycosides (eg. digoxin)
Indirectly increase intracellular calcium and cardiac contractility by inhibiting Na+/K+ ATPase
Digoxin is used in
Atrial fibrillation and CHF
Digoxin toxicity can be precipitated by
Antidote for digoxin toxicity
Digoxin immune fab
Drug used for moderate to severe heart failure, reduces mortality, especially for patients taking digitalis to prevent hypokalemia
Spironolactone, Eplerenone
Combination recommended for only African Americans to reduce preload and afterload in CHF
Isosorbide dinitrate/hydralazine
Beta 1 agonists used iv in acute decompensated HF
Dobutamine and dopamine
Diuretics work in CHF by
Reducing preload
Beta blockers work in CHF by
Reducing adverse effects of high catecholamine levels on heart (never use in acute heart failure)
Dual ARB and neprilysin inhibitor, early phase 2 trial for heart failure and hypertension
LCZ696, sucabitril
Select group of beta blockers that reduce heart failure mortality
Carvedilol, metoprolol, bisoprolol, nebivolol
Vasodilator used in acute CHF resembling brain natriuretic peptide
Nesiritide (Natrecor)
Vitamin K dependent anticoagulant
Warfarin (PT)
Warfarin is contraindicated in
Anticoagulant of choice in pregnancy
Heparin (PTT) increases activity of
Antithrombin 3
Route of administration of warfarin
Routes of administration of heparin
IV and IM (only LMW)
SE of both warfarin and heparin
SE of heparin
Heparin induced thrombocytopenia (HIT)
Alternative anticoagulant used if HIT develops
Antidote to reverse actions of warfarin
Vitamin K or fresh frozen plasma
Antidote to reverse actions of heparin
Protamine sulfate
MOA of aspirin
Irreversibly blocking cyclooxygenase
Agent used to treat MI and to reduce incidence of subsequent MI
Aspirin, metoprolol
SE of Aspirin
GI bleeding
Antiplatelet drug reserved for patients allergic to aspirin
SE for ticlopidine
Neutropenia and agranulocytosis
Effective in preventing TIA's
Clopidogrel and ticlopidine
Prevents thrombosis in patients with artificial heart valve
Block glycoprotein IIb/IIIa involved in platelet cross- linking
Abciximab, tirofiban and eptifibatide
MOA of thrombolytics
Degradation of fibrin clots and are administered IV
Thrombolytics are used for
Pulmonary embolism and DVT
Thrombolytic that can cause allergic reaction
Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA
Tissue plasmin activator
SE of tPA
Cerebral hemorrhage
Antidote for thrombolytics
Aminocaproic acid
Agent to treat hypochromic microcytic anemias
Ferrous sulfate
Chelating agent used in acute iron toxicity
Agent for pernicious anemia
Cyanocobalamin (Vit B12)
Agent used for neurological deficits in megaloblastic anemia
Vitamin B12
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
Folic acid
Agent used for anemias associated with renal failure
Erythropoietin agonists
Agent used neutropenia especially after chemotherapy
G-CSF (filgrastim) and GM-CSF (sargramostim)
Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy
Interleukin 11 (oprelvekin)
Drugs decrease intestinal absorption of cholesterol
Bile acid-binding resins
Cholestyramine and colestipol are
Bile acid-binding resins
Major nutritional side effect of bile acid-binding resins
Impair absorption of fat soluble vitamin absorption (A,D,E,K)
MOA of lovastatin (STATIN)
inhibits HMG COA reductase
HMG CoA reductase inhibitors are contraindicated in
MOA of drug or foods (grapefruit juice) that increase statin effect
Inhibit Cytochrome P450 3A4
SE of HMG COA reductase inhibitors
Rhabdomyolysis and Hepatotoxicity
Monitoring parameter to obtain before initiation of STATINS
Decreases liver triglycerol synthesis
SE of niacin
Cutaneous flush
Cutaneous flush can be reduced by pretreatment with
Fibrates (gemfibrozil) increase activity of
Lipoprotein lipase
Most common SE of fibrates
Fibrates are contraindicated in
Concurrent use of fibrates (gemfibrozil) and statins (simvastatin, lovastatin) increases risk of
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
Ezetimibe (Zetia)
inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)
Difference between aspirin and other NSAIDS
Aspirin irreversibly inhibits cyclooxygenase
Four main actions of NSAIDS
Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
Agent used for closure of patent ductus arteriosus
Aspirin is contraindicated in children with viral infection
Potential for development of Reye's syndrome
SE of salicylates
Tinnitus, GI bleeding
NSAID also available as an ophthalmic preparation
Diclofenac, ketoralac
NSAID available orally, IM and ophthalmically
NSAID that is used for acute condition, such as post- surgical pain and has limited duration (<5 days) of use due to nephrotoxicity
Newer NSAID that selectively inhibits COX-2
COX 2 inhibitors may have reduced risk of
Gastric ulcers and GI Bleeding
COX 2 inhibitors should be used cautiously in pts with
Pre-existing cardiac or renal disease
Acetaminophen only has
Antipyretic and analgesic activity
SE of acetaminophen
Antidote for acetaminophen toxicity Drugs-Modifying Anti-Rheumatic Agents (DMARDS)
DMARDs are slow acting drugs for
Rheumatic disease
Initial DMARD of choice for patients with RA
Drug ofter used in combination with TNF - alpha inhitors for RA
Causes bone marrow suppression
Interferes with activity of T-lymphocytes
Anti-malarial drug used in rheumatoid arthritis (RA)
SE of hydroxychloroquine
Retinal destruction and dermatitis
MOA of Leflunomide (newer agent)
Inhibiting dihydroorotate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T cell proliferation and decreased antibody production by B cells
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha)
Adalimumab, infliximab and etanercept
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
MOA of colchicine (used in acute gout)
Selective inhibitor of microtubule assembly
SE of colchicine
Kidney and liver toxicity, diarrhea
Agent used to treat chronic gout by increasing uric acid secretion and excretion
Probenecid and sulfinpyrazone
Allopurinol treats chronic gout by decreasing uric acid production by inhibiting
Xanthine oxidase
Rapid acting insulins that do not self-aggregate
lispro insulin, aspart insulin, glulisine insulin
Peakless long acting insulin
Insulin glargine
DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action
Decontamination of health care worker after caring for patient with C. difficile infection
Proper hand-washing with soap and water
Used to sterilize endoscopes and dental equipment
Formaldehyde, glutaraldehyde, ortho- phthalaldehyde, sterilox, hydrogen peroxide, peracetic acid
Disinfection of blood spills
1:10 dilution of household bleach
Bactericidal, fungicidal, sporicidal disinfectant used to wipe hospital beds
1:10 dilution of bleach, phenol