Pharmacology General Flashcards
Drugs with zero order elimination?
PEA– Phenytoin; Ethanol; Aspirin
Treat base overdoses with?
Amonium chloride
Phase 1 drug metabolism?
Reduction, oxidation, hydrolysis with cyp P450– usually yields slightly polar water soluble metabolites
Phase 2 metabolism?
Conjugation– glucuronidation; acetylation; sulfation
Efficacy vs potency?
Efficacy– maximal effect a drug can produce
Potency– amount of drug needed to produce an effect
Competitive antagonists shift curve?
To the right– decrease the potency (Diazepam+flumazenil on GABA)
Noncompetitive antagonist shifts curve?
Down– decreases efficacy
NE+phenoxybenzamine on alpha receptors
Partial agonist?
Reduce efficacy– potency can go up or down
therapeutic index?
Median lethal dose over median effective dose
Lineweaver burk plot– what happens if my point moves more to the right? i.e. greater x intercept?
The greater the Km and the lower the affinity
What happens if my x intercept gets smaller in the lineweaver burk plot?
Lower Km and higher affinity
Volume of distribution
Amount of drug in body/plasma drug concentration
Half life?
(.7*Vd)/Clearance
Adrenal medulla and sweat glands are innervated by?
Cholinergic fibers even though they are SYMPATHETIC
Muscarinic receptors are of what type?
GPCR (M1-M5)
Parasympathetics act on?
Cardiac and smooth muscle, glands, and nerve terminals
Mechanism of Gq?
Phospholipase c converts lipids into PIP2 which can go to
1) IP3–>inc Ca–>smooth muscle contraction
2) DAG–>protein kinase C
Mechanism of Gs/Gi?
Adenylyl cyclase converts ATP to cAMP–>protein kinase A which 1) blocks myosin light chain kinase and 2) increases Ca in heart
Qiss Qiq (till you’re) siq (of) Sqs?
alpha 1,2 beta1,2 M1,2,3 D1,D2 H1, H2 V1, v2
Increases vascular smooth muscle contraction?
alpha 1
increases pupillary dilator muscle?
alpha 1
Increases gastic acid secretion?
H2
Relaxes renal vascular smooth muscle?
D1
Dec insulin release? and dec lipolysis
alpha2
Increase insulin release? and inc lipolysis
beta2
Bronchodilation and tocolytic?
Beta 2
Ciliary muscle relaxation?
Beta 2
Increase platelet aggregation?
alpha 2
dec hr and contractility of atria?
M2
Increases lacrimal productoin (exocrine gland)?
M3
Increase bladder contraction?
M3
Bronchoconstriction?
M3
miosis and ciliary muscle contraction (i.e. accommodation)
M3
Pruritus?
H1
Intestinal and bladder sphincter muscle contraction?
alpha1
Epi effects blank more than blank?
Beta more than alpha