Pharmacology Flashcards
Km
proportional to 1/affininty of enzyme of substrate
Vmax
proportional to enzyme conc
Vd=
amount of drug in body/plasma conc
Clearance
rate of elimination of drug/plamsa drug conc: Vd*Ke (elimination constant)
Half life
t1/2=0.7*Vd/Clearance
Loading dose/maintenance dose
Loading dose=CpVd/F, Maintenance dose=CpCL*dosage interval/F
Amount of half lives to reach steady state
4-5 half lives
What is dosage interval constant and Cp constant
Dosage interval (time between doses), if not administered continuously Cp-target plasma concentration in steady state
3 drugs that have zero order elimination
Phenytoin, Ethanol, Aspirin
Treat weak acid overdose with?
Bicarbonate
Treat weak base overdose with?
Ammonium chloride
Phase geriatric patients lose first?
Phase I
Therapeutic index equation
TD50/TE50=median toxic tose/median effective dose
Drugs with lower therapeutic index
Digoxin, warfarin, lithium, theophylline “THEO, DIEGO went to WAR over LITHIUM”
Competitive antagonist example
Diazepam (agonist + flumazenil (competitive antagonist) on GABA receptor
Noncompetitive antagonist example
Norepinephrine (agonist) + phenoxybenzamine (noncompetitive antagonist on alpha receptor)
Example of partial agonist
Morphine (full agonist) vs. buprenorphine (partial agonist) at opioid mu receptors
Prevents ACh packaging in vesicles
Vesamicol
Prevents NE release for noradrenergic axon
a2 negative feedack, bretylium, guanethidine
Prevents tyrosine to DOPA conversion
metyrosine
Postoperative ileus, neurogenic ileus, urinary retention
Bethanechol
Constricts pupil and relieves intraocular pressure in glaucoma
Carbachol
Challenge test for diagnosis of asthma
Methacholine
Potent stimulator of sweat, tears, and saliva. Open- and closed angle glaucoma. Open angle constricts what and close angle constricts what?
Pilocarbine
Open-ciliary muscle contraction
Closed-pupillary sphincter muscle contraction
Alzheimer disease help increasing ACh
Donepezil, galantamine, rivastigmine
Diagnosis of myasthenia gravis
Edrophonium (extremely short acting
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade (post operative)
Neostigmine
AChe that penetrates CNS
Physostigmine
AChe that does not penetrate CNS
Neostigmine
When giving cholinomimetic agents, what 3 things do you have to watch out for exacerbation of
COPD, asthma, peptic ulcers
Organophosphate poisoning symptoms and what does it inhibit
Irreversible inhibits AChe
Diarrhea, Urination, Miosis, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation
Atropine vs Pralidoxime
Atroprine reverses muscaraninc effects but does not prevent development of nicotinic effects such as muscle paralysis
Pralidoxime is only medication that reverses both muscarininc and nicotinic effects of organophosphates
Produces mydriasis and cycloplegia
Atropine, homatropine, tropicamide
Treats acute dystonia in parkinson
Benztropine
Use parenterally: preoperative use to reduce airway secretions. Orally: drooling, peptic ulcer
Glycopyrrolate
Antispasmodic for irritable bowel syndrome
Hyoscyamine, dicyclomine
Used for COPD, asthma to help decrease bronchoconstriction
Ipratropium, tiotropium
Reduces bladder spasms and urge urinary incontinence (overactive bladder)
Oxybutynin, solifenacin, tolterodine
Used for motion sickness
Scopolamine
Atropine poisoning treatment
Physostigmine
Used to treat bradycardia and for ophthalmic applications
Atropine
Atropine effects on
Eye, airway, stomach, gut, bladder
Mydriasis+cycloplegia, decrease secretions, decrease acid production, decrease motility, decrease urgency in cystitis
Atropine toxicity
increase temp, dry, flushing, cycloplegia, disorientation
Consequence of mydriasis in atropine toxicity
angle-closure glaucoma
Hot feels cold and cold feels hot diagnosis
temperature related dysesthesia specific finding for ciguatoxin from ciguatera fish poisoning
Toxin that binds fast voltage-gated Na+ channels in cardiac and nerve tissue, preventing depolarization
Tetrodotoxin
MOA of patient with anaphylaxis like presentation who consumed dark meet fish and reasoning
Histidine in enteric system converted via bacterial histidine decarboxylase to histamine and histamine is not degraded by fish.
Used for acute asthma
Albuterol
Used for long term asthma and COPD control
Salmeterol
Albuterol, salmeterol receptor effect
B2>B1