01b: Pharmacology Flashcards
Lineweaver Burk: x-int approaches zero, affinity of enzyme to substrate (increases/decreases).
Decreases (Km increases)
Competitive inhibitors decrease (efficacy/potency) and noncompetitive inhibitors decrease (efficacy/potency).
Potency; efficacy
Small, hydrophilic compounds likely have (large/small) Vd and distributed mainly in (X) compartment.
Medium
X = ECF
Large, charged molecules likely have (large/small) Vd and distributed mainly in (X) compartment.
Small
X = intravascular (and bound to plasma proteins)
Drug infused at constant rate takes (X) number of half lives to reach steady state.
X = 4-5 (90% at 3.3 half lives)
Drugs: Loading dose calculation
(Cp)*(Vd)/(F)
Cp = target plasma conc at steady state F = bioavailability
Drugs: Maintenance dose calculation (not for continuous infusion)
(Cp)(CL)(𝝉)/(F)
Cp = target plasma conc at steady state 𝝉 = time between doses F = bioavailability
Time until drug reaches steady state is (increased/decreased) with increased (loading/maintenance) dose.
Independent of these! Depends primarily on half-life
Aspirin and acetaminophen drug interaction is an example of (X) effect
X = additive (their effect together is equal to sum of their individual effects)
Cortisol and catecholamine drug interaction is an example of (X) effect
X = permissive (cortisol required for full effects/responsiveness of catecholamines)
Clopidogrel and aspirin drug interaction is an example of (X) effect
X = synergistic (effects of them together is greater than sum of their individual effects)
Tachyphylactic drug interaction refers to which phenomenon?
Acute decrease in response to drug after initial/repeated administration
Zero-order kinetics: constant (X) of drug eliminated per unit time. List three examples of drugs eliminated in this manner.
X = amount
PEA (pea is round like 0)
Phenytoin, EtOH, Aspirin
First-order kinetics: constant (X) of drug eliminated per unit time. Applies to most drugs
X = fraction
Half-life (decreases/increases) in (zero/first)-order kinetics as concentration of drug decreases.
Decreases in zero order;
Remains constant in first-order
Aspirin overdose can be treated with (X), which will (ionize/neutralize) the urine and result in:
X = bicarbonate
Ionize (alkalinize)
Ionization of weak acid drugs (salicylate, phenobarbital, methotrexate) will trap it in urine and clear it quickly
What might be used to (ionize/neutralize) the urine and trap drugs that are weak bases, such as (X)?
Ammonium chloride;
Ionize (acidify) urine to then ionize and trap weak bases
X = amphetamines, TCAs
List the phases of drug metabolism. Star the one that geriatric patients lose first.
Phase I*: CYP450 (metabolites often still active)
Phase II: Conjugation (methylation, glucoronidation, acetylation, sulfation; inactive metabolites)
Why are patients that are slow acetylators at (increased/decreased) risk of drug side effects?
Increased
Decreased Phase II of drug metabolism (conjugation)
Drug efficacy is represented by (low/high) (X). Drug potency is represented by (low/high) (Y).
High; X = Vmax (max effect)
Low; Y = EC50 (amount of drug needed for given effect)
These two characteristics are unrelated
Give an example of partial agonism at the opioid mu receptor.
Morphine (full agonist) and buprenorphine (partial)
List four drugs that must be monitored carefully due to (low/high) therapeutic index.
Low (TD50/ED50)
Mnemonic: Warning! These Drugs are Lethal
- Warfarin
- Theophylline
- Digoxin
- Lithium
(X) glands are funky in that they’re part of (sympathetic/parasympathetic) pathway but innervated by (Y) fibers.
X = sweat (trying to remember these makes me sweat)
Sympathetic
Y = cholinergic
Botulinum toxin affects (muscarinic/nicotinic) ACh receptors. Repetitive nerve stimulation (can/cannot) increase compound muscle action potential
Both (since decreases ACh release from nerve terminals; cleaves SNARE proteins)
Can
T/F: Myasthenia gravis only affects nicotinic ACh receptors.
True
Activation of (X) receptor increases pupillary dilator muscle.
X = alpha1 (Gq class)
Activation of (X) adrenergic receptor(s) (increases/decreases) contraction of bladder and intestinal sphincters.
X = alpha1 (Gq class)
Increases
(X) adrenergic receptor plays important role in (increasing/decreasing) platelet aggregation.
X = alpha2 (Gi class)
Increasing
(X) adrenergic receptors play opposite roles in regulating aqueous humor production. They play similar roles in regulation of (Y).
X = beta2 (increases) and alpha2 (decreases) Y = insulin secretion and lipolysis
(X) adrenergic receptors play role in (increasing/decreasing) renin release.
X = beta1
Increasing
List the key receptors that work by Gq-protein-linked second messenger
Mnemonic: HAVe 1 M&M
H1, alpha1, V1 (vasopressin); M1, M3