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187 Cards in this Set

  • Front
  • Back
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)
Inducers of Cytochrome P450 (CYP450)
Barbiturates, phenytoin, carbamazepine, and rifampin
Inhibitors of CYP450
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Ability of drug to produce a biologic effect
Efficacy
Mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
MOA utilizes transmembrane receptors
Insulin
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
**
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine
Antidote used for heparin toxicity
Protamine Sulfate
**
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
**
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil
Interaction with this drug requires dose reduction of 6-MP
Allopurinol
**
May protect against doxorubicin cardio-toxicity by chelating iron
Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
Bleomycin
Binds tubulin and prevents the disassembly of microtubules during the M phase of the cell cycle inducing mitotic arrest
Paclitaxel (taxol)
**
Anti-estrogen used for estrogen receptor + breast cancer
Tamoxifen
**
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist
Odansetron, granisetron, dolasetron, palonosetron
Hormone inhibiting prolactin release
Dopamine
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Cosyntropin
**
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
**
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
PTU
PTU (propylthiouracil) MOA
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
Some side effects of corticosteroids
Hyperglycemia, Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
Diuretic used to antagonize aldosterone receptors
Spironolactone
Common SE of spironolactone
Gynecomastia and hyperkalemia
**
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)
Raloxifene
**
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
Diethylstilbestrol (DES)
Converted to more active form DHT by 5 alpha-reductase
Testosterone
Product of proinsulin cleavage used to assess insulin production
C-peptide
Long acting insulin
Ultralente (humulin U)
Amino acid derivative for treatment of Type II diabetes
Nateglinide
Increase bone density, also being tested for breast CA tx.
Raloxifene (SERM-selective estrogen receptor modulator)
**
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
Drug that causes contraction of the uterus
Oxytocin
Distribution of histamine receptors H1, H2, and H3
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
Prototype antagonist of H1 and H2 receptors
Diphenhydramine
1st generation antihistamine that is highly sedating
Diphendydramine
**
2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
H2 blocker that causes the most interactions with other drugs
Cimetidine
5HT-1D/1B agonist used for migraine headaches
Sumatriptan, naratriptan, and rizatriptan
**
Agents for reduction of postpartum bleeding
Oxytocin and ergonovine
**
Agents used in treatment of carcinoid tumor
Cyproheptadine
**
5HT-3 antagonist used in chemotherapeutic induced
emesis
Aprepitant, Ondansetron, granisetron,
dolasetron and palonosetron
***
Ergot alkaloid used as an illicit drug
LSD
Dopamine agonist used in hyperprolactinemia
Bromocriptine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Bradykinin
Drug causing depletion of substance P (vasodilator)
Capsaicin
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
Inhibitor of lipoxygenase
Zileuton
Used in pediatrics to maintain patency of ductus arteriosis
PGE1 (Alprostadil)
Prostaglandin used in the treatment impotence
PGE1 (Alprostadil)
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
Muscarinic antagonist used in asthma
Ipratropium
MOA action of cromolyn
Mast cell stabilizer
SE of long term (>5 days) corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
MOA of quinolones
Inhibit DNA gyrase
**
Drug used for MRSA
Vancomycin
Vancomycin MOA
Blocks peptidoglycan synthesis
**
Meningitis prophylaxis in exposed patients
Rifampin
Technique used to diagnose perianal itching, and the drug used to treat it
Scotch tape technique
and mebendazole
MOA of sulfonamides
Inhibit dihydropteroate synthase
Cheap wide spectrum antibiotic DOC of otitis media
Amoxicillin
**
DOC for tx of pseudomembranous colitis
Metronidazole
**
Anemia caused by trimethoprim
Megaloblastic anemia
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
Metronidazole
Treatment for TB patients (think RIPE)
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
Common side effect of Rifampin
Orange urine discoloration
DOC for influenza A and B
Oseltamivir or Zanamivir
DOC for RSV
Ribavirin
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Protease inhibitors
DOC for N. gonorrhea
Ceftriaxone
DOC for herpes and its MOA
Acyclovir; activates thymidine kinase
Anti-microbials that cause hemolysis in G6PD-deficient patients
Sulfonamides
Anti-biotic frequently used for chronic UTI prophylaxis
sulfamethoxazole/ trimethoprim
Major effect of benzodiazepines on sleep at high doses
REM is decreased
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Ethanol
System that increases in activity with chronic exposure and may contribute to tolerance
Microsomal ethanol oxidizing system MEOS
The most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
Drugs of choice for generalized tonic-clonic and partial seizures
Valproic acid, Phenytoin and Carbamazepine
Drugs of choice for absence seizures
Ethosuximide and valproic acid
Drug of choice for myoclonic seizures
Valproic acid
Anti-seizure drugs used also for pain of neuropathic orgin
Gabapentin
SE of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
Flumazenil
Opioid associated with awareness during surgery and post-operative recall, but still used for high-risk cardiovascular surgeries
Fentanyl
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
Dantrolene
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
Drug induced Parkinsonism
Side effects occuring in antipsychotics that block dopamine
EPS, hyperprolactinemia, amennorrhea, galactorrhea, neuroleptic malignant syndrome
Atypical antipsychotic causing high prolactin levels
Risperidone
Drug used in neuroleptic malignant syndrome
Dantrolene
Antipsychotics having the strongest autonomic effects
Chlorpromazine or Thioridazine
Agent with greater affinity to 5HT2A receptor; reserved for refractory schizophrenia, and can cause weight gain and agranulocytosis
Clozapine
Anti-psychotics shown not to cause tardive dyskinesia
Clozapine and quetiapine
Major route of elimination for Lithium
Kidneys
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
Lithium toxicity
DOC for bipolar affective disorder
Lithium
SE of lithium
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
TCA used in chronic pain, enuresis, and OCD
Imipramine
Unicyclic antidepressant least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
Bupropion
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release and pain transmission
Presynaptic mu, delta, and kappa receptors
Tolerance to all effects of opioid agonists can develop except
Miosis, convulsions and constipation
Opioid used in the management of withdrawal states
Methadone
Opioid available trans-dermally
Fentanyl
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
Morphine
Moderate opioid agonists
Codeine, hydrocodone, and oxycodone
Opioid antagonist that is given IV and had short DOA
Naloxone
Opioid antagonist that is given orally in alcohol dependency programs
Naltrexone
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
This agent may cause more severe, rapid and intense symptoms (abstinence syndrome) to a recovering addict
Naloxone
"Date rape drug"
Flunitrazepam (rohypnol)
These agents are CNS depressants
Ethanol, Barbiturates, and Benzodiazepines
Treatments available for nicotine addiction
Patches, gum, nasal spray, psychotherapy, and bupropion
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
Marijuana
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)
Treat manifestations of Parkinson's disease and EPS
Benztropine, trihexyphenidyl
Treatment of motion sickness
Scopolamine
Produce mydriasis and cycloplegia
Atropine, homatropine, and tropicamide
Bronchodilation in asthma and COPD
Ipratropium
Pneumonic for beta receptors
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
This is the drug of choice for anaphylactic shock
Epinephrine
These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion)
Alpha1 agonists
Alpha 1 agonist toxicity
Hypertension
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
Prazosin, terazosin, doxazosin
Selective B1 Receptor blockers that may be useful in treating cardiac conditions in patients with asthma
Acebutolol, atenolol, esmolol, metoprolol
This beta blocker lacks local anesthetic activity (decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
Timolol
These Beta blockers decrease aqueous secretion
Timolol (nonselective), betaxolol (selective)
Inhibit angiotensin-converting enzyme (ACE)
Ace inhibitors
Captopril and enalapril (-OPRIL ending) are
Ace inhibitors
SE of ACE inhibitors
Dry cough, hyperkalemia
Ace inhibitors are contraindicated in
pregnancy and with hyperkalemia
Losartan and valsartan block
Angiotensin receptor blockers (ARB)
Angiotensin receptor blockers do NOT cause
Dry cough
SE of CCB
Constipation, edema, and headache
Reduce heart rate, contractility, and O2 demand
Beta-blockers
Cardioselective Beta 1-blockers
Atenolol, acebutolol, and metoprolol
SE of beta blockers
Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
Alpha 1selective blockers
Prazosin, terazosin and doxazosin (-AZOSIN ending)
A1a-selective blocker used for BPH
Tamsulosin (Flomax)
SE of alpha blockers
Orthostatic hypotension (especially with first dose) and reflex tachycardia
Methyldopa is contraindicated in
Geriatrics due to its CNS (depression) effects
SE of hydralazine
Lupus-like syndrome
Diuretic used for mountain sickness and glaucoma
Acetazolamide
SE of acetazolamide
Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
Site of action of loop diuretics
Thick ascending limb
SE of loop (furosemide) diuretics
Hyperuricemia, hypokalemia and ototoxicity
Loops lose and thiazide diuretics retain
Calcium
Site of action of thiazide diuretics
Work at early distal convoluted tubule
SE of thiazide (HCTZ) diuretics
Hyperuricemia, hypokalemia and hyperglycemia
Potassium sparing diuretics inhibit
Na+/K+ exchange
Diuretic used to treat primary aldosteronism
Spironolactone
SE of spironolactone
Gynecomastia hyperkalemia, and impotence
Osmotic diuretic used for increased intracranial pressure
Mannitol
ADH agonist used for pituitary diabetes insipidus
Desmopressin (DDAVP)
MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
Sodium channel blockers
SE of procainamide
Lupus-like syndrome
Limiting side effect of Quinidine
Prolongs QT interval
DOC for management of acute Ventricular arrhythmias
Lidocaine
Life threatening cardiac event that prolong QT leads to
Torsades de pointes
MOA of sildenafil (Viagra)
Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
MOA of nitrates
Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
Vitamin K dependent anticoagulant
Warfarin (PT)
Heparin (PTT) increases activity of
Antithrombin 3
Antidote to reverse actions of heparin
Protamine sulfate
SE of Aspirin
GI bleeding
MOA of thrombolytics
Lyse thrombi by catalyzing the formation of plasmin which binds fibrin
Thrombolytics are used for
Pulmonary embolism and DVT
Agent for pernicious anemia
Cyanocobalamin (Vit B12)
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
Folic acid
Agent used for anemias associated with renal failure
Erythropoietin
Drug or foods (grapefruit juice) that increase statin effect
Inhibit Cytochrome P450 3A4
Monitoring parameter to obtain before initiation of STATINS
LFT's
Decreases liver triglycerol synthesis
Niacin
SE of niacin
Cutaneous flush
Fibrates (gemfibrozil) increase activity of
Lipoprotein lipase
Agent used for closure of patent ductus arteriosus
Indomethacin
Acetaminophen only has
Antipyretic and analgesic activity
Antidote for acetaminophen toxicity
N-acetylcysteine
DMARDs are slow acting drugs for
Rheumatic disease
NSAID used in gout
Indomethacin
Allopurinol treats chronic gout by inhibiting
Xanthine oxidase