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428 Cards in this Set
- Front
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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)
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* Half-life (T1/2)
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Relates the amount of drug in the body to the plasma concentration
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Volume of distribution (VD)
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Plasma concentration of a drug at a given time
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Cp
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The ratio of the rate of elimination of a drug to its plasma concentration
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Clearance (CL)
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The elimination of drug that occurs before it reaches the systemic circulation
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First pass effect
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The fraction of administered dose of a drug that reaches systemic circulation
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Bioavailability (F)
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When the rate of drug input equals the rate of drug elimination
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Steady state
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This step of metabolism makes a drug more hydrophilic and hence augments elimination
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* Phase I
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Different steps of Phase I
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Oxidation, reduction, hydrolysis
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Inducers of Cytochrome P450 (CYP450)
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* Barbiturates, phenytoin, carbamazepine, and rifampin
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Inhibitors of CYP450
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* Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione, sulfate
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Type of kinetics when a constant percentage of substrate is metabolized per unit time
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First order kinetics
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Drug elimination with a constant amount metabolized regardless of drug concentration
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Zero order kinetics
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Target plasma concentration x (volume of distribution divided by bioavailability)
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Loading dose (Cp*(Vd/F))
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Concentration in the plasma x (clearance divided by bioavailability)
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Maintenance dose (Cp*(CL/F))
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Strength of interaction between drug and its receptor
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Affinity
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Selectivity of a drug for its receptor
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Specificity
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Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
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Potency
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Maximum response achieveable from a drug
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* Efficacy
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Ability of a drug to produce 100% of the maximum response regardless of the potency
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Full agonist
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Ability to produce less than 100% of the response
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Partial agonist
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Ability to bind reversibly to the same site as the drug and without activating the effector system
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Competitive antagonist
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Class of drugs with ability to decrease the maximal response to an agonist
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Noncompetitive antagonist
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A hormone whose mechanism of action (MOA) utilizes intracellular receptors
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* Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors
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* Insulin
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Class of drugs whose MOA utilizes ligand gated ion channels
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Benzodiazepines and calcium channel blockers
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Median effective dose required for an effect in 50% of the population
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ED50
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Median toxic dose required for a toxic effect in 50% of the population
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TD50
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Dose which is lethal to 50% of the population
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LD50
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Window between therapeutic effect and toxic effect
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Therapeutic index
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Term for a high margin of safety
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High therapeutic index
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Term for a narrow margin of safety
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Low therapeutic index
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Antidote used for lead poisoning
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Dimercaprol, EDTA
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Antidote used for cyanide poisoning
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Nitrites
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Antidote used for anticholinergic poisoning
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Physostigmine
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Antidote used for organophosphate/anticholinesterase poisoning
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** Atropine, pralidoxime (2-PAM)
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Antidote used for iron salt toxicity
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Deferoxamine
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Antidote used for acetaminophen (APAP) toxicity
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* N-acetylcysteine (Mucomyst)
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Antidote for arsenic, mercury, lead, and gold poisoning
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Dimercaprol
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
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Penicillamine
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Antidote used for heparin overdose
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** Protamine
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Antidote used for warfarin toxicity
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* Vitamin K and Fresh frozen plasma (FFP)
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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** Aminocaproic acid
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Antidote used for methanol and ethylene glycol
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Ethanol or fomepizole
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Antidote used for opioid toxicity
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* Naloxone (IV), naltrexone (PO)
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Antidote used for benzodiazepine toxicity
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* Flumazenil
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Antidote used for tricyclic antidepressants (TCA)
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Sodium bicarbonate
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Antidote used for carbon monoxide poisoning
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100% O2 and hyperbaric O2
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Antidote used for digitalis toxicity
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Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
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Antidote used for beta agonist toxicity (eg. Metaproterenol)
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Esmolol
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Antidote for methotrexate toxicity
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Leucovorin
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Antidote for beta-blockers and hypoglycemia
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Glucagon
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Antidote useful for some drug induced Torsade de pointes
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Magnesium sulfate
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Antidote for hyperkalemia
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sodium polystyrene sulfonate (Kayexalate)
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Antidote for salicylate intoxication
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Alkalinize urine, dialysis
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Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
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Octreotide
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Somatotropin (GH) analog used in GH deficiency (dwarfism)
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Somatrem
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GHRH analog used as diagnostic agent
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Sermorelin
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GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
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Leuprolide
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GnRH antagonist with more immediate effects, used for infertility
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Ganirelix
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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
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* Bromocriptine
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Hormone inhibiting prolactin release
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* Dopamine
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ACTH analog used for diagnosis of patients with corticosteroid abnormality
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** Cosyntropin
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Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
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* Desmopressin (DDAVP)
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SE of OCs
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** Increased thromboembolic events
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Most widely used thyroid drugs such as Synthroid and Levoxyl contain
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** L-thyroxine (T4)
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T3 compound less widely used
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Cytomel
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Anti-thyroid drugs
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Thioamides, iodides, radioactive iodine, and ipodate
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Thioamide agents used in hyperthyroidism
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Methimazole and propylthiouracil (PTU)
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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
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* PTU
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PTU (propylthiouracil) MOA
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* Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
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Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
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Iodide salts
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Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
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** Thyroxine
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Permanently cures thyrotoxicosis , patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
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Radioactive iodine
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Radio contrast media that inhibits the conversion of T4 to T3
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Ipodate
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Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
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Beta-blockers such as propranolol
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Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
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Iron deiodinates thyroxine
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Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
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Estogens increase maternal TBG
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Used for Cushing's syndrome (increased corticosteroid)
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Dexamethasone suppression test
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Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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Aminoglutethimide
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Antifungal agent used for inhibition of all gonadal and adrenal steroids
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Ketoconazole
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Antiprogestin used as potent antagonist of GC receptor
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Mifepristone
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Diuretic used to antagonize aldosterone receptors
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* Spironolactone
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Common SE of spironolactone
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** Gynecomastia and hyperkalemia
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Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
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Estrogen
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Antiestrogen drugs used for fertility and breast cancer respectively
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Clomiphene and tamoxifen
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Common SE of tamoxifen and raloxifene
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Hot flashes
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Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
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** Raloxifene
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Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
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* Diethylstilbestrol (DES)
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Estrogen mostly used in oral contraceptives (OC)
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Ethinyl estradiol and mestranol
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Anti-progesterone used as abortifacient
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Mifepristone (RU-486)
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Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
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Combination oral contraceptives (OC)
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Oral contraceptive available in a transdermal patch
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Ortho-Evra
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Converted to more active form DHT by 5 alphareductase
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* Testosterone
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5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
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Finasteride (Proscar and Propecia respectively)
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Anabolic steroid that has potential for abuse
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Nandrolone, oxymetholone, and oxandrolone
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Anti-androgen used for hirsutism in females
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Cyproterone acetate
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Drug is used with testosterone for male fertility
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** Leuprolide
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Disease caused by excess ergot alkaloids
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St. Anthony's Fire
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Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
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Autocoids
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Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
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Zollinger-Ellison Syndrome
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Drug that causes contraction of the uterus
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* Oxytocin
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Distribution of histamine receptors H1, H2, and H3
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* Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
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Prototype antagonist of H1 and H2 receptors
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* Diphenhydramine and cimetridine, respectively
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1st generation antihistamine that is highly sedating
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** Diphendydramine
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1st generation antihistamine that is least sedating
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Chlorpheniramine or cyclizine
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2nd generation antihistamines
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* Fexofenadine, loratadine, and cetirizine
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Generation of antihistamine that has the most CNS effects
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First generation due to being more lipidsoluble
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Major indication for H1 receptor antagonist
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Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety and insomnia and is not addictive
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hydroxyzine (Atarax)
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H1 antagonist used in motion sickness
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Dimenhydrinate, meclizine, and other 1st generation
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Most common side effect of 1st generation antihistamines
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Sedation
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Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 isoenzyme.
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Terfenadine and astemizole (have been removed from the market)
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H2 blocker that causes the most interactions with other drugs
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* Cimetidine
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Clinical use for H2 blockers
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Acid reflux disease, duodenal ulcer and peptic ulcer disease
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Receptors for serotonin (5HT-1) are located
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Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
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5HT-1d agonist used for migraine headaches
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** Sumatriptan, naratriptan, and rizatriptan
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Triptan available in parenteral and nasal formulation
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Sumatriptan
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H1 blocker that is also a serotonin antagonist
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Cyproheptadine
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Agents for reduction of postpartum bleeding
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** Oxytocin, ergonovine and ergotamine
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Agents used in treatment of carcinoid tumor
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** Ketanserin cyproheptadine, and phenoxybenzamine
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5HT-3 antagonist used in chemotherapeutic induced emesis
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*** Ondansetron, granisetron, dolasetron and alosetron
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5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
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Dolasetron
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DOC to treat chemo-induced nausea and vomiting
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** Odansetron
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Drug used in ergot alkaloids overdose, ischemia and gangrene
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Nitroprusside
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Reason ergot alkaloids are contraindicated in pregnancy
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Uterine contractions
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SE of ergot alkaloids
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Hallucinations resembling psychosis
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Ergot alkaloid used as an illicit drug
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* LSD
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Dopamine agonist used in hyperprolactinemia
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* Bromocriptine
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Peptide causing increased capillary permeability and edema
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Bradykinin and histamine
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Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
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* Bradykinin
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Drug causing depletion of substance P (vasodilator)
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* Capsaicin
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Prostaglandins that cause abortions
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* Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
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Difference between COX 1 and COX 2
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COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
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Drug that selectively inhibits COX 2
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Celecoxib and rofecoxib
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Inhibitor of lipoxygenase
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* Zileuton
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Major SE of zileuton
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Liver toxicity
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Inhibitor of leukotrienes (LTD4) receptors and used in asthma
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Zafirlukast and montelukast
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Used in pediatrics to maintain patency of ductus arteriosis
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* PGE1
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Approved for use in severe pulmonary HTN
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PGI2 (epoprostenol)
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Prostaglandin used in the treatment of impotence
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* Alprostadil
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Irreversible, nonselective COX inhibitor
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Aspirin
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Class of drugs that reversibly inhibit COX
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NSAIDS
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Primary endogenous substrate for Nitric Oxidase Synthase
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Arginine
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MOA and effect of nitric oxide
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* Stimulates cGMP which leads to vascular smooth muscle relaxation
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Long acting beta 2 agonist used in asthma
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Salmeterol
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Muscarinic antagonist used in asthma
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* Ipratropium
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MOA action of cromolyn
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* Mast cell stabilizer
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Methylxanthine derivative used as a remedy for intermittent claudication
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Pentoxifylline
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MOA of corticosteroids
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inhibit phospholipase A2
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SE of long term (>5 days) corticosteroid therapy and remedy
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* Adrenal suppression and weaning slowly, respectively
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Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
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* Ethanol
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Agent with zero-order kinetics
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Ethanol
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Rate limiting step of alcohol metabolism
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Aldehyde dehydrogenase
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System that increases in activity with chronic ethanol exposure and may contribute to tolerance
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* MEOS
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Enzyme that metabolizes acetaldehyde to acetate
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Aldehyde dehydrogenase
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Agents that inhibit acetaldehyde dehydrogenase
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Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
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Agent that inhibits alcohol dyhydrogenase and its clinical use
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FOMEPIZOLE – used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
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Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
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Disulfiram
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The most common neurologic abnormality in chronic alcoholics
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* Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
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Agent that is teratogen and causes a fetal syndrome
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Ethanol
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Agent that is the antidote for methanol overdose
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Ethanol, fomepizole
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Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
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Fomepizole
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MOA of general anesthetics
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Most are thought to act at GABA-A receptor - chloride channel
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Inhaled anesthetic with a low blood/gas partition coefficient
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Nitrous oxide
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Inversely related to potency of anesthetics
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Minimum alveolar anesthetic concentration (MAC)
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Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
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Halothane and methoxyflurane
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Most inhaled anesthetics SE
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Decrease arterial blood pressure
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Inhaled anesthetics are myocardial depressants
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Enflurane and halothane
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Inhaled anesthetic causes peripheral vasodilation
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Isoflurane
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Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
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Halothane
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Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
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Nitrous oxide
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Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
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Methoxyflurane
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Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
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Nitrous oxide
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Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
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Desflurane
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DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
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* Dantrolene
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IV barbiturate used as a pre-op anesthetic
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Thiopental
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Benzodiazepine used adjunctively in anesthesia
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Midazolam
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Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
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* Flumazenil
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This produces "dissociative anesthesia ", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
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Ketamine
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Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
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* Fentanyl
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State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
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Neuroleptanesthesia
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Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
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Propofol
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MOA of local anesthetics (LA's)
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Block voltage-dependent sodium channels
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This may enhance activity of local anesthetics
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Hyperkalemia
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This may antagonize activity of local anesthetics
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Hypercalcemia
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Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
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Vasodilation
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Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
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Cocaine
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Longer acting local anesthetics which are less dependent on vasoconstrictors
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Tetracaine and bupivacaine
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These LA's have surface activity
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Cocaine and benzocaine
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Most important toxic effects of most local anesthetics
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CNS toxicity
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Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
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Cocaine
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LA causing methemoglobinemia
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Prilocaine
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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
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Neuromuscular blocking drugs
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These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
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Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
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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)
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Nondepolarizing type antagonists
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Agent with long duration of action and is most likely to cause histamine release
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Tubocurarine
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Non-depolarizing skeletal muscle antagonist that has short duration
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Mivacurium
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Skeletal muscle agent that can block muscarinic receptors
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Pancuronium
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Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
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Atracurium
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One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
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Succinylcholine
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During Phase I these agents worsen muscle
paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine |
Cholinesterase inhibitors
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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
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Facilitates GABA presynaptic inhibition
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Diazepam
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GABA agonist in the spinal cord
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Baclofen
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Similar to clonidine and may cause hypotension
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Tizanidine
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DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
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* Dantrolene
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Agent used for acute muscle spasm
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Cyclobenzaprine
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Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
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Older antipsychotic agents, D2 receptors
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MOA of neuroleptics
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Dopamine blockade
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Side effects occuring in antipsychotics that block dopamine
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* Hyperprolactinemia, menorrhea,
galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain |
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Antipsychotics that reduce positive symptoms only
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Older antipsychotics
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Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
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Olanzapine, aripiprazole, and sertindole
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Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
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* Risperidone
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Atypical antipsychotic causing high prolactin levels
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* Risperidone
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Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
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Olanzapine
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Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
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Haloperidol
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Drug used in neuroleptic malignant syndrome
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* Dantrolene
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Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
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Muscarinic blockers
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Antipsychotic having the strongest autonomic effects
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* Thioridazine
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Antipsychotic having the weakest autonomic effects
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Haloperidol
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Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits,
and high doses have been associated with ventricular arrhythmias |
Thioridazine
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Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
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**Clozapine
|
|
|
Anti-psychotic not shown to cause tardive dyskinesia
|
* Clozapine
|
|
|
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
|
Quetiapine
|
|
|
Major route of elimination for Lithium
|
* Kidneys
|
|
|
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
*Lithium toxicity
|
|
|
Drug that increases renal clearance of and hence decreases levels of lithium
|
Theophylline
|
|
|
Lithium is associated with this congenital defect
|
Cardiac anomalies and is contraindicated in pregnancy or lactation
|
|
|
DOC for bipolar affective disorder
|
* Lithium
|
|
|
Concern using lithium
|
Low therapeutic index
|
|
|
SE of lithium
|
* Tremor, sedation, ataxia, aphasia, thyroid
enlargement, and reversible diabetes insipidus |
|
|
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
|
Meperidine
|
|
|
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
|
* Methadone
|
|
|
Opioid available trans-dermally
|
* Fentanyl
|
|
|
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
|
* Morphine
|
|
|
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
|
Meperidine
|
|
|
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
|
Propoxyphene
|
|
|
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
|
Buprenorphine
|
|
|
Opioid antagonist that is given IV and had short DOA
|
* Naloxone
|
|
|
Opioid antagonist that is given orally in alcohol dependency programs
|
* Naltrexone
|
|
|
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
|
Steroids
|
|
|
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
|
* Naloxone
|
|
|
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
|
Caffeine
|
|
|
W/D from this drug causes anxiety and mental discomfort
|
Nicotine
|
|
|
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
|
Amphetamines
|
|
|
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
|
PCP
|
|
|
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
|
* Marijuana
|
|
|
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
|
* Ipratropium
|
|
|
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 pneumonic for anticholinergic toxicity
|
dry as a bone, red as a beet, mad as a
hatter, hot as a hare, blind as a bat |
|
|
Atropine fever is the most dangerous effect and can be lethal in this population group
|
Infants
|
|
|
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
|
Succinylcholine
|
|
|
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
|
|
|
Pneumonic for beta receptors
|
* You have 1 heart (Beta 1) and 2 lungs (Beta 2)
|
|
|
This is the drug of choice for anaphylactic shock
|
* Epinephrine
|
|
|
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
|
Amphetamines
|
|
|
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
|
Phenylephrine
|
|
|
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
|
Albuterol
|
|
|
Longer acting Beta 2 agonist is recommended for prophylaxis of asthma
|
Salmeterol
|
|
|
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
|
Midodrine
|
|
|
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
|
Terbutaline
|
|
|
Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses
|
Epinephrine
|
|
|
Mast cells to reduce release of hisamine and inflammatory mediators
|
Epinephrine
|
|
|
Agent used in shock because it dilates coronary arteries and increases renal blood flow
|
Dopamine
|
|
|
Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
|
Dobutamine
|
|
|
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
|
Ephedrine
|
|
|
Alpha 1 agonist toxicity
|
* Hypertension
|
|
|
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
|
|
|
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
|
* Timolol
|
|
|
This parenteral beta blocker is a short acting (minutes)
|
Esmolol
|
|
|
This beta blocker is the longest acting
|
Nadolol
|
|
|
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
|
Propranolol
|
|
|
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
|
Acetazolamide
|
|
|
This agent cause increased aqueous outflow
|
Prostaglandin PGF2a
|
|
|
ADH agonist used for pituitary diabetes insipidus
|
* Desmopressin (DDAVP)
|
|
|
Used for SIADH
|
Demeclocycline
|
|
|
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
|
* Amiodarone
|
|
|
DOC for digoxin induced arrhythmias
|
Phenytoin
|
|
|
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
|
B-blockers
|
|
|
Antiarrhythmic that exhibits Class II and III properties
|
Sotalol
|
|
|
Side effect of sotalol
|
prolongs QT and PR interval
|
|
|
Used intravenously for acute arrhythmias during surgery
|
Esmolol
|
|
|
Anti-arrhythmics that decrease mortality
|
B-blockers
|
|
|
MOA of class III antiarrhythmics
|
Potassium channel blockers
|
|
|
Class III antiarrhythmic that exhibits properties of all 4 classes
|
Amiodarone
|
|
|
Specific pharmacokinetic characteristic of amiodarone
|
Prolonged half-life, up to six weeks
|
|
|
Antiarrhythmic effective in most types of arrhythmia
|
Amiodarone
|
|
|
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 leads to
|
* Torsades de pointes
|
|
|
Agent to treat torsades de pointes
|
Magnesium sulfate
|
|
|
Drug used supraventricular arrhythmias
|
Digoxin
|
|
|
DOC for paroxysmal supraventricular tachycardia (PSVT)
|
Adenosine
|
|
|
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
|
Adenosine
|
|
|
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
|
Tolerance
|
|
|
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
|
Classic
|
|
|
Vitamin K dependent anticoagulant
|
* Warfarin (PT)
|
|
|
Warfarin is contraindicated in
|
Pregnancy
|
|
|
Anticoagulant of choice in pregnancy
|
Heparin
|
|
|
Heparin (PTT) increases activity of
|
* Antithrombin 3
|
|
|
Route of administration of warfarin
|
Oral
|
|
|
Routes of administration of heparin
|
IV and IM (only LMW)
|
|
|
SE of both warfarin and heparin
|
Bleeding
|
|
|
SE of heparin
|
Heparin induced thrombocytopenia (HIT)
|
|
|
Alternative anticoagulant used if HIT develops
|
Lepirudin
|
|
|
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
|
Ticlopidine
|
|
|
SE for ticlopidine
|
Neutropenia and agranulocytosis
|
|
|
Effective in preventing TIA's
|
Clopidogrel and ticlopidine
|
|
|
Prevents thrombosis in patients with artificial heart valve
|
Dipyridamole
|
|
|
Block glycoprotein IIb/IIIa involved in platelet crosslinking
|
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
|
Streptokinase
|
|
|
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
|
Deferoxamine
|
|
|
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
|
|
|
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
|
Pregnancy
|
|
|
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
|
* LFT's
|
|
|
Decreases liver triglycerol synthesis
|
* Niacin
|
|
|
SE of niacin
|
* Cutaneous flush
|
|
|
Cutaneous flush and be reduced by pretreatment with
|
Aspirin
|
|
|
Fibrates (gemfibrozil) increase activity of
|
* Lipoprotein lipase
|
|
|
Most common SE of fibrates
|
Nausea
|
|
|
Fibrates are contraindicated in
|
Pregnancy
|
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
|
Ezetimibe (Zetia)
|
|
|
DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action
|
Adenosine
|
