Pharmacology Flashcards
In Michaelis-Menten enzyme kinetics, what is the Km?
Km is the concentration of substrate [S] at 1/2 of the Vmax of the enzyme. Km is inversely related to the affinity of the enzyme for its substrate.
In Michaelis-Menten enzyme kinetics, Vmax is directly proportional to what?
Enzyme concentration
What is a Lineweaver-Burk plot?
Basically the Michaelis-Menten kinetics plot but inversed: x intercept is 1/[S], y intercept is 1/V
What is the formula to calculate T1/2 (half-life)?
(0.693 x Vd) / CL
What is the formula to calculate clearance?
CL = (rate of elimination of drug)/(plasma drug concentration) = Vd x Ke *Ke is elimination constant
What is the formula to calculate Loading dose?
(Cp x Vd) / F
What is the formula to calculate Maintenance dose?
(Cp x CL x tau) / F *tau is the dosage interval
Opioid analgesics lead to what cellular events?
Opening of K channels and closing of Ca channels
What are CYP 450 inducers?
Carbamazepine, phenobarbital, phenytoin, rifampin, griseofulvin
What are CYP 450 inhibitors?
Cimetidine, ciprofloxacin, erythromycin, azole antifungals, grapefruit juice, isoniazid, ritonavir
Which receptors are linked to Gs proteins?
beta1, beta2
Which receptors are linked to Gi/o proteins?
M2, alpha2, CB1, GABAb
Which receptors are linked to Gq proteins?
alpha1, M1, M3
What is zero-order elimination?
Rate of elimination is constant regardless of Cp
What is first-order elimination?
Rate of elimination is directly proportional to the drug concentration. Cp decreases exponentially with time
Overdose with drugs that are weak acids are treated by making the urine more basic or more acidic?
Alkalinize the urine with bicarbonate (trapped in the ionized form)
Overdose with drugs that are weak bases are treated by making the urine more basic or more acidic?
Acidify the urine with ammonium chloride
Are amphetamines weak bases or acids?
Weak bases
Is aspirin a weak base or weak acid?
Weak acid
What is Phase I drug metabolism?
Reduction, oxidation, hydrolysis with cytochrome P450 usually yields slightly polar, water-soluble metabolites (often still active)
What is Phase II drug metabolism?
Conjugation (glucuronidation, acetylation, sulfation) usually yields very polar, inactive metabolites (renally excreted)
What is the antidote to acetaminophen?
N-acetylcysteine (replenishes glutathione)
What is the antidote to AChE inhibitors, organophosphates?
Atropine followed by pralidoxime
What is the antidote to amphetamines?
NH4Cl (acidify urine)
What is the antidote to antimuscarinics, anticholinergic agents?
Physostigmine salicylate, control hyperthermia
What is the antidote to benzodiazepines?
Flumazenil
What is the antidote to beta-blockers?
Glucagon
What is the antidote to carbon monoxide?
100% O2, hyperbaric O2
What is the antidote to copper, arsenic, gold?
Penicillamine
What is the antidote to cyanide?
Nitrite + thiosulfate, hydrocobalamin
What is the antidote to digitalis?
Anti-digitalis Fab fragments
What is the antidote to heparin?
Protamine sulfate
What is the antidote to iron?
Deferoxamine, deferasirox
What is the antidote to lead?
EDTA, dimercaprol, succimer, penicillamine
What is the antidote to mercury, arsenic, gold?
Dimercaprol (BAL), succimer
What is the antidote to methanol, ethylene glycol?
Fomepizole > ethanol, dialysis
What is the antidote to methemoglobin?
Methylene blue, vitC
What is the antidote to opioids?
Naloxone
What is the antidote to salicylates?
NaHCO3 (alkalinize the urine), dialysis
What is the antidote to TCAs?
NaHCO3 (plasma alkalinization)
What is the antidote to tPa, streptokinase, urokinase?
Aminocaproic acid
What is the antidote to warfarin?
Vitamin K, plasma if active bleeding
Which drugs can cause coronary vasospasm?
Cocaine, supatriptan, ergot alkaloids
Which drugs can cause cutaneous flushing?
Vancomycin, adenosine, niacin, CCBs
Which drugs can cause dilated cardiomyopathy?
Doxorubicin and daunorubicin (anthracyclines - chemo)
Which drugs can cause torsades de pointes?
Class III and class IA antiarrhythmics, macrolides, antipsychotics, TCAs
Which drugs can cause adrenocortical insufficiency?
Glucocorticoids
Which drug can cause acute cholestatic hepatitis, jaundice?
Erythromycin
Which drugs can cause focal to massive hepatic necrosis?
Halothane, Amanita phalloides, valproic acid, acetaminophen: “liver HAVAc”
Which drugs can cause pseudomembranous colitis?
Clindamycin, ampicillin, cephalosporins
Which drugs can cause agranulocytosis?
Dapsone, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthiouracil “Drugs CCCrush Myeloblasts and Promyelocytes”
Which drugs can cause aplastic anemia?
Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil: “Can’t Make New Blood Cells Properly”
Which drugs can cause direct Coombs-positive hemolytic anemia?
Methyldopa, penicillin
Which drug can cause gray baby syndrome?
Chloramphenicol
Which drugs can cause thrombocytopenia?
Heparin, cimetidine
Which drugs can cause thrombotic complications?
OCPs
Which drugs can cause gingival hyperplasia?
Phenytoin, verapamil, cyclosporine, nifedipine
Which drugs can cause hyperuricemia (gout)?
Pyrazinamide, Thiazides, Furosemide, Niacin, Cyclosporine: “Painful Tophi and Feet Need Care”
Which drugs can cause myopathy?
Fibrates, niacin, colchicine, hydroxychloroquine, interferon-alpha, penicillamine, statins, glucocorticoids
Which drugs can cause osteoporosis?
Corticosteroids, heparin
Which drugs can cause photosensitivity?
Sulfonamides, Amdiodarone, Tetracyclines, 5-FU: “SAT For Photo”
Which drugs can cause rash (Steven-Johnson syndrome)?
Anti-epileptic drugs (ethosuximide, carbamazepine, lamotrigine, phenytoin, phenobarbital), Allopurinol, Sulfa drugs, Penicillin: “Steven Johnson has epileptic Allergy to Sulfa drugs and Penicillin”
Which drugs can cause SLE-like syndrome?
Sulfa drugs, Hydralazine, INH, Procainamide, Phenytoin, Etanercept
Which drugs can cause teeth discoloration?
Tetracyclines
Which drugs can cause tendonitis, tendon rupture, and cartilage damage?
Fluoroquinolones
Which drugs can cause cinchonism?
Quinidine, quinine
Which drugs can cause Parkinson-like syndrome?
Antipsychotics, reserpine, metoclopramide
Which drugs can cause seizures?
INH (VitB6 deficiency), bupropion, imipenem/cilastatin, tramadol, eflurane, metoclopramide
Which drugs can cause tardive dyskinesia?
Antipsychotics, metoclopramide
Which drugs can cause diabetes insipidus?
Lithium, demeclocycline
Which drugs can cause Fanconi syndrome?
Expired tetracycline
Which drugs can cause hemorrhagic cystitis?
Cyclophosphamide, ifosfamide
Which drugs can cause interstitial nephritis?
Methicillin, NSAIDs, furosemide
Which drugs can cause SIADH?
Carbamazepine, cyclophosphamide, SSRIs
Which drugs can cause a dry cough?
ACE-Is
Which drugs can cause pulmonary fibrosis?
Bleomycin, amiodarone, busulfan, methotrexate
Which drugs can cause antimuscarinic effects?
Atropine, TCAs, H1-blockers, antipsychotics
Which drugs can cause disulfiram-like reaction?
Metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st gen sulfonylureas
Which drugs can cause nephrotoxicity/ototoxicity?
Aminoglycosides, vancomycin, loop diuretics, cisplatin
What are the sulfa drugs?
Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine, Sulfonylureas: “Popular FACTSSS”
What happens when someone with a sulfa allergy takes a sulfa drug?
Fever, UTI, Stevens-Johnson syndrom, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria (hives)
Drug names ending in -azole are what category?
Ergosterol synthesis inhibitors
Drug names ending in -bendazole are what category?
Antiparasitic/antihelmintic
Drug names ending in -cillin are what category?
Peptidoglycan synthesis inhibitors
Drug names ending in -cycline are what category?
Protein synthesis inhibitors
Drug names ending in -ivir are what category?
Neuraminidase inhibitors
Drug names ending in -navir are what category?
PIs (HIV)
Drug names ending in -ovir are what category?
DNA polymerase inhibitor
Drug names ending in -thromycin are what category?
Macrolides
Drug names ending in -ane are what category?
Inhalational general anesthetic
Drug names ending in -azine are what category?
Typical antipsychotic
Drug names ending in -barbital are what category?
Barbiturates
Drug names ending in -caine are what category?
Local anesthetic
Drug names ending in -etine are what category?
SSRIs
Drug names ending in -ipramine are what category?
TCAs
Drug names ending in -triptan are what category?
5-HT 1B/1D agonists
Drug names ending in -triptyline are what category?
TCAs
Drug names ending in -zepam are what category?
Benzodiazepines
Drug names ending in -zolam are what category?
Benzodiazepines
Drug names ending in -chol are what category?
Cholinergic agonists
Drug names ending in -curium or -curonium are what category?
Non-depolarizing paralytic
Drug names ending in -olol are what category?
Beta-blockers
Drug names ending in -stigmine are what category?
AChE-Inhibitors
Drug names ending in -terol are what category?
Beta2 agonists
Drug names ending in -zosin are what category?
Alpha1 antagonists
Drug names ending in -afil are what category?
PDE-5 inhibitors
Drug names ending in -dipine are what category?
Dihydropyridine CCB
Drug names ending in -pril are what category?
ACE-Inhibitors
Drug names ending in -sartan are what category?
Angiotensin II receptor antagonists
Drug names ending in -statin are what category?
HMG-CoA reductase inhibitor
Drug names ending in -dronate are what category?
Bisphosphonate
Drug names ending in -glitazone are what category?
PPAR-gamma activator
Drug names ending in -prazole are what category?
PPIs
Drug names ending in -prost are what category?
PG analog
Drug names ending in -tidine are what category?
H2 antagonists
Drug names ending in -tropin are what category?
Pituitary hormone
Drug names ending in -ximab are what category?
Chimeric monoclonal Ab
Drug names ending in -zumab are what category?
Humanized monoclonal Ab
What is DRESS syndrome?
‘Drug Reaction with Eosinophilia and Systemic Symptoms’ - Rare, life-threatening, 2-8 weeks after exposure, usually happens with anticonvulsants, allopurinol, sulfonamides, and antibiotics. Likely involves drug-induced herpesvirus reactivation followed by clonal expansion of T cells that cross-react with drug. Fever, lymphadenopathy, facial edema, diffuse morbilliform skin rash.
Dopamine1 Receptor is associated with which receptor?
Gs - relaxes renal vasculature smooth muscle
Dopamine2 Receptor is associated with which receptor?
Gi - modulates transmitter release, esp in brain
Histamine1 Receptor is associated with which receptor?
Gq - Increases nasal and bronchial mucus production, increases vascular permeability, contraction of bronchioles, pruritis, pain
Histamine2 Receptor is associated with which receptor?
Gs - Increased gastric acid secretion
Vasopressin1 Receptor is associated with which receptor?
Gq - Increases vascular smooth muscle contraction
Vasopressin2 Receptor is associated with which receptor?
Gs - Increase water permeability and reabsorption in the collecting tubules of the kidney (V2 is found in the 2 kidneys)
OD with AChE-inhibitors can be treated with what?
Pralidoxime (regenerates AChE) - peripheral only - atropine blocks parasympathetic NS peripherally and centrally