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70 Cards in this Set

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Vd equation
Vd = (amount of drug in body)/(plasma drug concentration)
Low Vd
distributes to blood
Medium Vd (8-60L)
distributes to extracellular space
High Vd (60+L)
distributes to tissues
Loading dose equation
Cp x (Vd/F)
Maintenance dose equation
Cp x (CL/F)
Change in loading dose and maintenance dose w/ impaired renal or hepatic function
loading dose remains the same, but maintenance dose decreases
Drugs w/ zero-order elimination
Phenytoin, Ethanol, Aspirin
Weak acid drugs
phenobarbitol, MTX, TCAs, aspirin
Treat overdose w/ bicarbonate in order to deprotonate them so that they can't escape the environment
Weak base drugs
amphetamines
Treat overdose w/ ammonium chloride to protonate them so they can't leave the environment
Phase I metabolism
reduction, oxidation, hydrolysis by P450 enymes
Phase II metabolism
acetylation, glucuronidation, sulfation to yield poloar, inactive metabolites that can be renally excreted
Therapeutic index
LD50/ED50
High therapeutic index is a good thing because it means that effective dose is low and lethal dose is relatively higher than the effective dose
Sweat gland innervation
Sympathetic
Muscarinic ACh postsynaptic fibers
Cardiac, smooth muscle, gland, and nerve cell sympathetic innervation
NE (alpha or beta adrenergic)
Renal vascular smooth muscle innervation
sympathetic
D1 agonist
Skeletal muscle innervation
somatic
Nicotininc ACh postsynaptic fibers
Cardiac, smooth muscle, gland, and nerve cell parasympathetic innervation
muscarinic ACh postsynaptic fibers
All preganglionic fibers are...
Nicotinic ACh
a1 adrenergic
increases vascular smooth muscle contraction, mydriasis, increases intestinal and bladder sphincter muscle contraction
a2 adrenergic
decreases sympathetic outflow, decreases insulin release
B1 adrenergic
increases heart rate, contractility, renin release, lipolysis
B2 adrenergic
B1 + vasodilation, bronchodilation, insulin release, decrease in uterine tone
M1 cholinergic
CNS, enteric nervous system
M2 cholinergic
decrease heart rate and contractility of atria
M3 cholinergic
increase exocrine gland secretion, gut peristalsis, bladder contraction, bronchoconstriction, miosis, accomodation
D1 dopaminergic
relaxes renal vascular smooth muscle
D2 dopaminergic
modulates transmitter release in brain
H1 histaminergic
increases mucus production in nasal and bronchial, bronchoconstriction, pruritis, pain, vasodilation, vasopermeability
H2 histaminergic
increases gastric acid secretion
V1 vasopressinergic
vasoconstriction
V2 vasopressinergic
reabsorption of kidney H20
Q g-protein mechanism
activates phospholipase C, which cleaves lipids into PIP2. PIP2 then is cleaved into IP3 and DAG. IP3 directly increases calcium, while DAG activates protein kinase C
Hemicholinium
prevents reuptake of choline into the presynaptic nerve terminal
Vesamicol
prevents packaging of ACh into presynaptic vesicles
Metyrosine
inhibits conversion of tyrosine into DOPA
Reserpine
VMAT inhibitor
Guanethidine
prevents NE vesicles from fusing w/ the presynaptic nerve terminal
Amphetamine
increases release of NE from the presynaptic nerve terminal
pilocarpine
used in glaucoma and dry mouth
resistant to AChE
Neostigmine uses
ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade
Cholinesterase poisoning
Parathion and organophosphates
Oxybutynin analog
glycopyrrolate: used to reduce urinary urgency and mild cystitis and reduce bladder spasms
Methscopolamine analogs
Pirenzepine, propantheline: used to PUD treatment
Atropine S/E in ederly, BPH, infants
elderly: acute angle-closure glaucoma. BPH: urinary retention. Infant: hyperthermia
Hexamethonium
nicotinic antagonist that acts as a ganglionic blocker. leads to severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction
Low dose of epinephrine
selective for B1, similar to dobutamine
Indirect general sympathomimetic agonists
amphetamine, ephedrine, cocaine
Tx of HTN w/ renal disease
clonidine, methldopa
Mirtazapine
presynaptic a2 blocker used in treating depression
S/E: sedation, increased serum cholesterol, increases appetite
Side effects of beta blockers
impotence, exacerbation of asthma, AV block, sedation, hyperlipidemia (metoprolol) and masking of hypoglycemic episodes
Partial B-agonists
pindolol, acebutolol
contraindicated in angina because they have sympathomimetic properties
B1-selective antagonists
Acebutolol, betaxolol, esmolol, atenolol, metoprolol (A BEAM)
Treatment of digoxin overdose
Anti-Dig Fab, normalize K+, Mg2+, lidocaine
Iron overdose tx
deferoxamine
Lead overdose tx
EDTA, dimercaprol, succimer, penicillamine
Mercury, arsenic, gold overdose tx
dimercaprol
Copper, arsenic, gold overdose tx
penicillamine
Methanol, ethylene glycol tx
Ethanol, fomepizole
Drugs that cause cutaneous flushing
vancomycin, adenosine, niacin, Ca2+ blockers
Drugs that cause agranulocytosis
clozapine, carbamazepine, colchicine, propylthiouracil, methimazole, dapsone
Drug that causes acute cholestatic hepatitis
Macrolides
Drugs that cause hot flashes
clomiphene, tamoxifen
Drugs that cause hypothyroidism
lithium, amiodarone
Drugs that cause gout
furosemide, thiazides, niacin
Drugs that cause photosensitivity
sulfonamides, amiodarone, tetracycline, 5-FU
Drug induced lupus
"Q CHIMPP": quinidine, chlorpromazine, hydralazine, isoniazid, methyldopa, penicillamine, procainamide
anti-histone antibodies
Cinchonism
caused by quinidine, quinine
tinnitus, dizziness, occasional fainting
Nephrotoxicity/Ototoxicity
aminoglycosides, vancomycin, loop diuretics, cisplatin
Overdose of methanol tx
folate (induces formic acid conversion to CO2), fomepizole, ethanol