General Pharm Flashcards
Common CYP 450 inducers (increase metabolism of other drugs)
"Most Chronic alcoholics Steal Phen-Phen and Never Refuse Greasy Carbs" Modafinil Chronic alcohol use St. John's wort Phenytoin Phenobarbital Nevirapine Rifampin Griseofulvin Carbamazepine
Common CYP 450 inhibitors (decrease metabolism/increase serum concentration and toxicity of other drugs)
"SICKFACES.COM when i Am drinking Grapefruit juice" Sodium valproate INH Cimetidine Ketoconazole Fluconazole Acute alcohol abuse Chloramphenicol Erythro/clarithromycin Sulfonamides Ciprofloxacin Omeprazole Metronidazole Amiodarone Grapefruit juice
Equation for maintenance dose
maintenance dose = (dose required for steady state) * CL/[bioavailability fraction]
(bioavailability fraction = 1 if given IV)
Half life equation
t1/2 = Vd*0.7 / CL
Equation for loading dose
Vd * (dose required for steady state) / [bioavailability fraction]
(bioavailability fraction = 1 if given IV)
Phase I metabolism
Reduction, Oxidation, Hydrolysis (“R-OH”). Geriatric pts lose phase I first. CYP450 responsible for most Phase I rxns; also converts pro-carcinogens into carcinogens that can cause mutations in human DNA
slightly polar, water soluble, often active metabolites
Phase II metabolism
“Geriatric pts have More GAS”
Methylation, Glucuronidation, Acetylation, Sulfation
very polar, inactive metabolites (renally excreted)
GPCR pathways for various receptor types
- HAVe 1 M&M: H1, alpha1, V1, M1 & M3 receptors follow Gq pathway (PLC –> IP3/DAG –> increased Ca2+ –> SM contrxn)
- MAD 2’s: M2, alpha2, D2 receptors follow Gi pathway (reduce cAMP –> increased MLCK activation –> SM relax
- all else (beta1/2/3, D1, H2, V2): Gs pathways (increased cAMP, increased PKA, Ca2+ in heart –> contraction
Drugs that increase risk of osteoporosis
Corticosteroids (decrease bone formation)
Depot medoxyprogesterone acetate, Aromatase inhibitors (decreased E)
GnRH agonists (reduced T & E)
Anticonvulsants that induce CYP450 - phenobarb, phenytoin, carbamazepine (increased vit D breakdown)
Heparin (stimulates clasts/suppresses blasts)
PPI’s (decrease Ca2+ reabsorption)
Equilibrium potential of Na+, K+, Cl-, Ca2+ and resting membrane potential
Na+ = +60 mV (into cell) K+ = -90 mV (out of cell) Cl- = -75 mV (into cell) Ca2+ = +125 mV (into cell) (resting potential = -70 mV)
Equation for bioavailability (F) of a drug administred non-IV route
F = (AUC oral)(dose IV) / (AUC IV)(dose oral)
Qualities of drugs that are preferentially processed by the liver vs. the kidney
High lipophilicity and high Vd. These drugs have good CNS penetration and are preferentially by the liver into more polar compounds for easier elimination in bile and urine. These drugs are poorly eliminated by kidney as they will rapidly cross tubular membranes after filtration to reenter tissues