Pharm One Liners High Yield Flashcards
Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
Half-life (T1/2)
Rifampin, phenobarbital, phenytoin, carbamazepine, St. Johns wort
Inducers of CYP450 (particularly CYP3A4)
Ritonavir (protease inhibitors), cimetadine, macrolides, ketoconazole (azoles), quinidine, amiodarone, grapefruit juice
Inhibitors of CYP450 (particularly CYP3A4)
Ability of drug to produce the maximal biologic effect
Efficacy
Mechanism of action utilizes intracellular receptors
Steroid and hormones
Mechanism of action utilizes transmembrane receptors that have intrinsic enzymatic activity
Insulin, EGF, TGFbeta, PDGF, ANP
Antidote for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote acetaminophen poisoning
N-acetylcysteine
Antidote used for heparin toxicity
Protamine sulfate
Antidote used for warfarin toxicity
Vitamin K1 and fresh frozen plasma
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote for opioid toxicity
Naloxone (IV)
Antidote for benzodiazepine toxicity
Flumazenil
Antidote for methotrexate toxicity
Leucovorin
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
Bethanechol
Toxicity of cholinergics
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
Antimuscarinic that treats Parkinsonism and extrapyramidal disease
Benztropine, trihexyphenidyl
Antimuscarinic for the treatment of motion sickness
Scopolamine
Produce mydriasis and cycloplegia
Atropine, anti-muscarinics
Antimuscarinic that causes bronchodilation in asthma and COPD
Ipratropium, tiotropium
Its ability to vasoconstrict and increase blood pressure makes it useful as local decongestant and for the therapy of spinal shock (temporary maintenance of blood pressure)
Alpha 1 agonists
Alpha 1 agonist toxicity
Hypertension
Selective alpha 1 blocker used for hypertension, benign prostatic hyperplasia, may cause first dose orthostatic hypotension
Prazosin, terazosin, doxazosin
Alpha 1a-selective blocker used for benign prostatic hyperplasia
Tamsulosin
Side effect of alpha blockers
Orthostatic hypotension (especially with first dose) and reflex tachycardia
Selective beta 1 receptor blockers useful for treating cardiac conditions in patients with asthma
Acebutolol, betaxolol, esmolol, atenolol, metoprolol (A BEAM)
Non-selective beta blocker that lacks local anesthetic activity, indicated for glaucoma
Timolol
Side effects of beta blockers
Bradycardia, AV block, impotence, dyslipidemia, exacerbation of COPD
Beta blockers’ effect on the heart in antianginal therapy
Reduce heart rate, blood pressure, contractility, and increase end-diastolic volume
Captopril and enalapril (-PRIL ending) are
ACE inhibitors
Side effects of angiotensin converting enzyme inhibitors
Dry cough, hyperkalemia, angioedema
Inactivated by angiotensin converting enzyme, contributes to dry cough and angioedema
Bradykinin
Angiotensin converting enzyme inhibitors are contraindicated in
Pregnancy, hyperkalemia
Mechanism of action of losartan and valsartan
Block Angiotensin II Type 1 (AT1) Receptors
Side effect associated with angiotensin converting enzyme inhibitors but not angiotensin receptor blockers
Dry cough
Calcium channel blockers with predominate effect on arteriole dilation
Nifedipine, amlodipine, nimodipine (dihydropyridines)
Calcium channel blockers with predominant effect on the heart
Verapamil, diltiazem (non-dihydropyridines)
Side effects of calcium channel blockers
Constipation, peripheral edema, cardiac depression, AV block
Alpha 2 agonist used in pregnant women with hypertension
Methyldopa
Methyldopa is contraindicated in
Geriatrics due to its CNS (depression) effects
Side effect of hydralazine
Lupus-like syndrome
MOA and effect of nitric oxide
Stimulates cGMP, leads to vascular smooth muscle relaxation
Mechanism of action of sildenafil
Inhibits phosphodiesterase-5, which keeps it from degrading cGMP (allowing for smooth muscle relaxation and vasodilation)
Mechanism of action of organic nitrates
Requires an enzymatic process to form NO, relaxes vascular smooth muscle of veins
Mechanism of action of class I antiarrhythmics
Sodium channel blockers
Mechanism of action of class III antiarrhythmics
Potassium channel blockers
Limiting side effect of class Ia and III antiarrhythmics
Prolongs QT interval
Most common side effects of quinidine that limits its use
Cinchonism
Side effect of procainamide
Systemic lupus-like syndrome
Drug of choice for management of acute ventricular tachycardia
Amiodarone
Side effects of Amiodarone
Thyroid dysfunction, corneal deposits, liver damage and pulmonary fibrosis
Life threatening cardiac event that prolong QT leads to
Torsades de pointes
Mechanism of action of statins
inhibits HMG COA reductase
Two side effects of HMG COA reductase inhibitors
Rhabdomyolysis and Hepatotoxicity
Two parameters to obtain before initiation of statins
LFT’s, creatine kinase
How grapefruit juice increases statin effect
Inhibit CYP450 3A4
Fibrates increase activity of
Lipoprotein lipase
Mechanism of action involves indirect reduction of liver triglyceride synthesis
Niacin, fibrates
Side effects of niacin
Cutaneous flush
Side effect of aspirin
GI bleeding
Vitamin K dependent anticoagulant with zero-order kinetics of elimination
Warfarin (PT)
Heparin (PTT) increases activity of
Antithrombin 3
Specific side effect of heparin
Heparin induced thrombocytopenia (HIT)
Mechanism of action of thrombolytics
Lyse thrombi by catalyzing the formation of plasmin which cleaves fibrin
Indications for thrombolytics
Pulmonary embolism, severe deep vein thrombosis
Diuretic used as prophylactic for mountain sickness and glaucoma
Acetazolamide
Side effects of acetazolamide
Alkalization of the urine (precipitate Ca salts), metabolic acidosis, hypokalemia, paresthesias, and encephalopathy in patients with hepatic impairment
Site of action of loop diuretics
Thick ascending limb (NKCC channel)
Side effects of loop diuretics
Hyperuricemia, hypokalemia, metabolic alkalosis and ototoxicity (also hyperglycemia and hypocalcemia)
An electrolyte that is lost in the urine by acute treatment with loop diuretics but can be retained by thiazides
Calcium
Site of action of thiazide diuretics
Early distal convoluted tubule (Na-Cl Symporter)
Side effects of thiazide diuretics
Hyperuricemia, hypokalemia, metabolic alkalosis, hyperlipidemia, and hyperglycemia (also hypercalcemia)
Mechanism of action of amiloride
Inhibit epithelial sodium channels (ENaC) in the distal convoluted tubules and collecting duct
Diuretic used to treat primary aldosteronism
Spironolactone, eplerenone
Side effect of spironolactone
Gynecomastia, hyperkalemia, and impotence
Diuretic used to reduce intracranial pressure
Mannitol
Antidiuretic hormone analog used for central diabetes insipidus and nocturnal enuresis
Desmopressin
Cheap wide spectrum antibiotic drug of choice for otitis media
Amoxicillin
Drug of choice for N. gonorrhea
Ceftriaxone
Drug used for MRSA
Vancomycin
Mechanism of action of vancomycin
Binds D-Ala-D-Ala on murein monomers and prevent polymerization of the murein monomers
Drug of choice for giardia, entamoeba, pseudomembranous colitis (C. Diff.), and trichomonas
Metronidazole
Drug of choice for treatment of mild to moderate pseudomembranous colitis
Metronidazole
Mechanism of action of fluoroquinolones
Inhibit DNA gyrase (topoisomerase II) and topoisomerase IV
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
Anemia caused by trimethoprim
Megaloblastic anemia
Anti-bacterials that cause hemolysis in G6PD-deficient patients
Sulfonamides
Mechanism of action of sulfonamides
Inhibit dihydropteroate synthase
Quadruple therapy for the treatment of tuberculosis
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
Meningitis prophylaxis in exposed patients
Rifampin
Common side effect of Rifampin
Orange urine discoloration
Technique used to diagnose perianal itching, and the drug used to treat it
Scotch tape technique (Pinworm test - Enterobius vermicularis); mebendazole (can also use albendazole)
Drug of choice for influenza A and B
Oseltamivir or Zanamivir
Drug of choice for respiratory syncytial virus (RSV)
Ribavirin
Drug of choice for herpes and its mechanism of action
Acyclovir; activated by viral thymidine kinase, inhibits viral DNA replication
Anti-retroviral class that causes drug interactions by causing inhibition of CYP enzymes
Protease inhibitors
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol), PGE2, and PGF2alpha
Prostaglandin analog used as 2nd line for erectile dysfunction
Alprostadil (PGE1)
Prostaglandin analog used in pediatrics to maintain patency of ductus arteriosis
Alprostadil (PGE1)
NSAID that may be used for closure of patent ductus arteriosus
Indomethacin
Two main actions of acetaminophen
Antipyretic and analgesic activity
Inhibitor of lipoxygenase
Zileuton
Agent that inhibits xanthine oxidases and used to treat chronic gout
Allopurinol, febuxostat
DMARDs are slow acting drugs for this indication
Rheumatic diseases
1st line for rheumatoic arthritis for most patients
Low-dose methotrexate
Dose-limiting toxicity of methotrexate
Myelosuppression
Drug for treating malignant hyperthermia associated with drug-drug interaction between halogenated anesthetics and depolarizing neuromuscular blocker (succinylcholine)
Dantrolene
Mechanism of action of cromolyn
Prevent mast cell degranulation (by blocking opening of Cl- channels)
Ergot dopamine agonist used to suppress prolactin release
Bromocriptine
Synthetic human corticotropin used for diagnosis of adrenal insufficiency
Cosyntropin
Agent used to stimulate uterine contraction and labor, milk letdowns, and control postpartum bleeding
Oxytocin
Agent of choice for the treatment of hypothyroidism
Levothyroxine (T4)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and indicated for pregnant women in 1st trimester
Propylthiouracil (PTU)
Propylthiouracil (PTU) mechanism of action
Inhibits thyroid peroxidase
Side effects of corticosteroids
Iatrogenic Cushing’s syndrome, hyperglycemia, impaired wound healing, osteoporosis, peptic ulcers, myopathy, adrenal suppression (> 2 week treatment)
Intermediate-acting insulin with variable pharmacokinetics; use is mostly replaced by long-acting insulin
Neutral protamine Hagedorn (NPH) insulin
First line drug for the treatment of type 2 diabetes
Metformin
Most serious side effect of metformin
Lactic acidosis
May be used intranasally to decreases bone resorption
Calcitonin (salmon prep)
Selective estrogen receptor modulator most commonly used for the treatment of breast cancer
Tamoxifen
Selective estrogen receptor modulator used for prevention of osteoporosis and invasive breast cancer
Raloxifene
Androgen receptor agonist used to treat hypogonadism and promote secondary sex characteristics
Testosterone
Distribution of histamine receptors H1, H2, and H3
Smooth muscle and mast cells; stomach, heart, and mast cells; nerve endings, CNS respectively
1st generation antihistamine that is highly sedating
Diphendydramine
Three 2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
H2 antagonist that causes the most interactions with other drugs
Cimetidine
5HT-1A receptor partial agonist indicated for generalized anxiety disorder; due to longer onset of action, is less effective for acute anxiety
Buspirone
5HT-1D/1B agonist used for migraine headaches
Sumatriptan and -triptans
H1 antihistamine with 5HT2 antagonist activity that is mostly used for carcinoid tumor but may be used to treat serotonin syndrome
Cyproheptadine
5HT-3 antagonist used for the prevention of chemotherapy-induced nausea and vomiting
Ondansetron and -setrons
Three beta blockers that decrease aqueous production
Timolol (nonselective), betaxolol (selective), carteolol (nonselective)
Prostaglandin 2 alpha analog used to increase aqueous humor outflow
Latanoprost
Mechanism of action of benzodiazepines
Increase frequency of GABA-mediated chloride ion channel (GABAA) opening
Mechanism of action of barbiturates
Increase duration of GABAA chloride channel opening
Three nonbenzodiazepine hypnotics that lack suppressive effect on REM and are preferred over benzodiazepines for the treatment of insomnia
Zolpidem, zaleplon, eszopiclone
Drug of choice for treatment of acute status epilepticus
Diazepam, lorazepam
Drug of choice for partial seizures
Carbamazepine
Drugs of choice for generalized tonic-clonic seizures
Carbamazepine, phenytoin, valproic acid
Antiepileptic agent that exhibits zero-order kinetics, causes fetal hydantoin syndrome, and induces CYP450
Phenytoin
Side effects of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
Drug of choice for myoclonic seizures that may also be used for absence seizures
Valproic acid
Drug of choice for absence seizures
Ethosuximide
Antiepileptic drug used also for pain of neuropathic orgin
Gabapentin
Mechanism of action of opioids on analgesia
Activate mu receptors to 1. close presynaptic Ca2+ channels to inhibit neurotransmitter release, 2. open postsynaptic K+ channels to hyperpolarize cell membrane
Tolerance to all effects of opioid agonists can develop except
Miosis, constipation
Opioid that can be given PO, IV, IM, and intrathecal to relieve anxiety associated with pulmonary edema
Morphine
Opioid available trans-dermally
Fentanyl
Long-acting opioids used for the management of withdrawal states (these drugs are used for pts with an opioid addiction)
Methadone, buprenorphine
Moderate opioid agonists
Codeine, hydrocodone, and oxycodone
Opioid antagonist that is given IV
Naloxone
Opioid antagonist that is given orally
Naltrexone
Rare, but fatal side effect associated with combination of halogenated inhalation anesthetic and depolarizing neuromuscular blocker (succinylcholine)
Malignant hyperthermia
Opioid safe for use of analgesia and anesthesia during cardiac surgery
Fentanyl
Produces dissociative anesthesia but has significant analgesic activity
Ketamine
Precursor of dopamine that can cross the blood-brain-barrier and used to alleviate motor dysfunction in Parkinson’s disease
Levodopa (L-dopa)
Inhibits peripheral DOPA decarboxylase, reduces peripheral side effects of dopamine precursor and enhances its delivery to the brain
Carbidopa
Inhibits monoamine oxidase type B (MAO-B), used as monotherapy for early or mild Parkinson’s disease or adjunct to improve motor function in patients with fluctuations in clinical response
Selegiline
Three main classes of CNS depressant drugs of abuse
Alcohol, opioid, barbiturate/benzodiazepine
Agent that is metabolized by alcohol dehydrogenase or microsomal ethanol-oxidizing system (MEOS) to acetaldehyde; displays zero-order kinetics of elimination
Ethanol
Enzyme that is induced through chronic exposure to alcohol, may contribute to tolerance
Microsomal ethanol oxidizing system (MEOS)
Neurological abnormality caused by chronic alcohol use and thiamine deficiency
Wernicke-Korsakoff syndrome
Respiratory and CNS depression, pinpoint pupils, seizures, and needle track marks are symptoms of this intoxication
Opioid
Opioid receptor antagonist that is used to treat opioid intoxication, may cause more rapid and intense symptoms of withdrawal
Naloxone
Two date rape drugs that work through enhancement of GABA receptors in the brain
Flunitrazepam, GHB (γ-hydroxybutyrate)
Benzodiazepine antagonist used to treat benzodiazepine intoxication
Flumazenil
Treatments available for nicotine addiction
Patch, gum, lozenge, bupropion, varenicline
Synthetic ergot derivative that can produce perceptual hallucinations and used as an illicit drug; may cause paranoia
LSD (lysergic acid diethylamide)
Active ingredient is tetrahydrocannabinol (THC); side effects include impairment of judgment, altered sense of time, increased appetite, and hallucinations
Marijuana
Primary mechanism of action of typical antipsychotics
Inhibits D2 receptors
Common endocrine side effects of all typical antipsychotic drugs
Hyperprolactinemia, galactorrhea
Common side effects of low potency typical antipsychotic drugs
Dry mouth (anticholinergic), sedation (antihistamine), hypotension (α1 block)
Side effects more commonly associated with high potency typical antipsychotic drugs
Extrapyramidal symptoms: Dystonia (continuous spasms/muscle contractions), Akathisia (motor restlessness), Bradykinesia (slow movement), Tardive Dyskinesia (irregulary, jerky movements - typically in the face)
Life-threatening side effect associated with typical antipsychotic drugs
Neuroleptic malignant syndrome
Treatment for drug-induced neuroleptic malignant syndrome
Dantrolene
Primary mechanism of action of atypical antipsychotics
Inhibit 5-HT2 receptors
Atypical antipsychotic that can produce potentially fatal agranulocytosis and increase incidence of seizures
Clozapine
Three life-threatining side effects associated with tricyclic antidepressants
Convulsion, cardiotoxocity, coma (3 C’s)
Serious side effect of selective serotonin reuptake inhibitors when used with other drugs such as monoamine oxidase inhibitors, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressants
Serotonin Syndrome
Antidepressant that non-selectively inhibits neuronal reuptake; less likely to cause sedation, autonomic, cardiovascular, or sexual dysfunction; also used for smoking cessation
Bupropion
Antidepressant that inhibits serotonin reuptake but also antagonizes 5HT-2 receptors; causes priapism
Trazodone
First line drug for classic bipolar disorder with euphoric mania
Lithium
Side effects of lithium
Tremor, hypothyroidism, nephrogenic diabetes insipidus, fetal cardiac defects
Antineoplastic folic acid analog that inhibits dihydrofolate reductase
Methotrexate
Two antineoplastics that require dose-reduction in patients who are taking allopurinol
Azathioprine, 6-mercaptopurine
Hyperstabilizes microtubule polymer and prevents microtubule breakdown
Paclitaxel, -taxels
Nitrosureas that spontaneously form active intermediates that cross-link DNA; can cross blood-brain-barrier and is indicated for brain tumors
Carmustine, -mustines, streptozocin
Iron-chelator that is used to protect against anthracycline-induced cardio-toxicity
Dexrazoxane
DNA intercalating agent with minimal myelosuppression that induces formation of free radicals; dose-limiting side effects include pulmonary fibrosis and mucocutaneous reactions
Bleomycin
Agent used for megaloblastic anemia (but does not reverse neurologic symptoms) and decrease neural tube defects during pregnancy
Folic acid
Agent used for pernicious anemia
Cyanocobalamin (Vit B12)
Agent used for anemias (especially with renal failure)
Erythropoietin