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192 Cards in this Set
- Front
- Back
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Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
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Half-life (T1/2)
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This step of metabolism makes a drug more hydrophilic and hence augments elimination
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Phase I
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Inducers of Cytochrome P450 (CYP450)
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Barbiturates, phenytoin, carbamazepine, rifampin, St. John's Wort
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Inhibitors of CYP450
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Amiodarone, Diltiazem, Verapamil, Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
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Maximum response achieveable from a drug
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Efficacy
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A hormone whose mechanism of action (MOA) utilizes intracellular receptors
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Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors
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Insulin
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Antidote used for organophosphate/anticholinesterase poisoning
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Atropine, pralidoxime (2-PAM)
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine (Mucomyst)
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Antidote used for heparin overdose
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Protamine
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Antidote used for warfarin toxicity
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Vitamin K and Fresh frozen plasma (FFP)
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid
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Antidote used for opioid toxicity
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Naloxone (IV), naltrexone (PO)
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Antidote used for benzodiazepine toxicity
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Flumazenil
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Interaction with this drug requires dose reduction of 6- MP
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Allopurinol
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Iron-chelating agent, protects against doxorubicin toxicity by scavenging free radicals
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Dexrazoxane
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Blows DNA (breaks DNA strands), limiting SE is pulmonary toxicity
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Bleomycin
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Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
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Paclitaxel (taxol)
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Anti-estrogen used for estrogen receptor + breast cancer
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Tamoxifen
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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
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Bromocriptine
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Hormone inhibiting prolactin release
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Dopamine
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ACTH analog used for diagnosis of patients with corticosteroid abnormality
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Cosyntropin
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Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
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Desmopressin (DDAVP)
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SE of OCs
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Increased thromboembolic events
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Most widely used thyroid drugs such as Synthroid and Levoxyl contain
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L-thyroxine (T4)
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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
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PTU
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PTU (propylthiouracil) MOA
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Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
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Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
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Thyroxine
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Some side effects of corticosteroids
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Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
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Common SE of spironolactone
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Gynecomastia and hyperkalemia
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Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
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Diethylstilbestrol (DES)
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Converted to more active form DHT by 5 alpha- reductase
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Testosterone
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Drug is used with testosterone for male fertility
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Leuprolide
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Product of proinsulin cleavage used to assess insulin production
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C-peptide
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Exogenous insulin contains
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No C-peptide
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Amino acid derivative, active as an insulin secretagogue
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Nateglinide
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Increase bone density, also being tested for breast CA prophlaxis
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Raloxifene (SERM-selective estrogen receptor modulator)
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Used intranasally and decreases bone resorption
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Calcitonin (salmon prep)
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Drug that causes contraction of the uterus
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Oxytocin
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Distribution of histamine receptors H1, H2, and H3
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Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
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Prototype antagonist of H1 and H2 receptors
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Diphenhydramine and cimetidine, respectively
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1st generation antihistamine that is highly sedating
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Diphendydramine
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2nd generation antihistamines
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Fexofenadine, loratadine, and cetirizine
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H2 blocker that causes the most interactions with other drugs
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Cimetidine
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5HT-1d agonist used for migraine headaches
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Sumatriptan, naratriptan, and rizatriptan
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Agents for reduction of postpartum bleeding
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Oxytocin, ergonovine and ergotamine
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Agents used in treatment of carcinoid tumor
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Ketanserin cyproheptadine, and phenoxybenzamine
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5HT-3 antagonist used in chemotherapeutic induced emesis
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Ondansetron, granisetron, dolasetron and alosetron
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DOC to treat chemo-induced nausea and vomiting
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Odansetron
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Ergot alkaloid used as an illicit drug
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LSD
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Dopamine agonist used in hyperprolactinemia
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Bromocriptine
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Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
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Bradykinin
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Drug causing depletion of substance P (vasodilator)
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Capsaicin
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Prostaglandins that cause abortions
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Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
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Inhibitor of lipoxygenase
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Zileuton
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Used in pediatrics to maintain patency of ductus arteriosis
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PGE1
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Prostaglandin used in the treatment of impotence
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Alprostadil
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MOA and effect of nitric oxide
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Stimulates cGMP which leads to vascular smooth muscle relaxation
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Muscarinic antagonist used in asthma
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Ipratropium
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MOA action of cromolyn
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Mast cell stabilizer
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SE of long term corticosteroid therapy and remedy
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Adrenal suppression and weaning slowly, respectively
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MOA of quinolones
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Inhibit DNA gyrase
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Drug used for MRSA
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Vancomycin
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Vancomycin MOA
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Blocks cell wall synthesis by sequestration
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Meningitis prophylaxis for persons in contact with patients
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Ciprofloxacin or Rifampin (for children less than 4 yrs old)
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Technique used to diagnose perianal itching, and the drug used to treat it
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Scotch tape technique and mebendazole
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MOA of sulfonamides
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Inhibit dihydropteroate synthase
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Cheap wide spectrum antibiotic DOC for otitis media
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Amoxicillin
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DOC for tx of pseudomembranous colitis (mild)
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Metronidazole
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Anemia caused by trimethoprim
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Megaloblastic anemia
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DOC for giardia, bacterial vaginosis, and trichomonas
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Metronidazole
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Treatment for TB patients (think RIPE)
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R ifampin, I soniazid, P yrazinamide, and E thambutol
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Drug used for N. gonorrhea in females
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Ceftriaxone
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DOC for herpes and its MOA
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Acyclovir; phosphorylation, incorporation into viral DNA, and chain termination
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Anti-bacterials that cause hemolysis in G6PD- deficient patients
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Sulfonamides
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Anti-biotic frequently used for chronic UTI prophylaxis
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sulfamethoxazole/ trimethoprim
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DOC for influenza A
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Oseltamivir
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DOC for severe RSV
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Ribavirin
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HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
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Protease inhibitors
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Major effect of benzodiazepines on sleep at high doses
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REM is decreased
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Reason benzos are used cautiously in pregnancy
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Ability to cross the placenta
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Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
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Flumazenil
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Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
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Ethanol
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System that increases in activity with chronic ethanol exposure and may contribute to tolerance
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MEOS
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The most common neurologic abnormality in chronic alcoholics
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Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
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Drugs of choice for generalized tonic-clonic and partial seizures
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Valproic acid and Phenytoin
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Drugs of choice for absence seizures
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Ethosuximide and valproic acid
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Drug of choice for myoclonic seizures
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Valproic acid
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Anti-seizure drugs used also for pain of neuropathic origin
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Gabapentin
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SE of phenytoin
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Gingival hyperplasia, nystagmus, diplopia and ataxia
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DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
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Dantrolene
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Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
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Flumazenil
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Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
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Fentanyl
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DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
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Dantrolene
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Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
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Drug induced Parkinsonism
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Side effects occuring in antipsychotics that block dopamine
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Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
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Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
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Risperidone
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Atypical antipsychotic causing high prolactin levels
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Risperidone
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Drug used in neuroleptic malignant syndrome
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Dantrolene
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Antipsychotic having the strongest autonomic effects
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Thioridazine
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Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
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Clozapine
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Anti-psychotic not shown to cause tardive dyskinesia
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Clozapine
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Major route of elimination for Lithium
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Kidneys
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Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
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Lithium toxicity
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DOC for bipolar affective disorder
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Lithium
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SE of lithium
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Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
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TCA used in chronic pain, enuresis, and ADD
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Imipramine
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Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
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Bupropion
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Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
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Presynaptic mu, delta, and kappa receptors
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Tolerance to all effects of opioid agonists can develop except
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Miosis and constipation
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Opioid used in the management of withdrawal states
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Methadone
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Opioid available trans-dermally
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Fentanyl
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Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
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Morphine
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Moderate opioid agonists
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Codeine, hydrocodone, and oxycodone
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Opioid antagonist that is given IV and had short DOA
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Naloxone
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Opioid antagonist that is given orally in alcohol dependency programs
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Naltrexone
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Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
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Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
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This agent may cause more severe, rapid and intense symptoms to a recovering addict
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Naloxone
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"Date rape drug"
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Flunitrazepam (rohypnol)
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These agents are CNS depressants
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Ethanol, Barbiturates, and Benzodiazepines
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Treatments available for nicotine addiction
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Patches, gum, nasal spray, psychotherapy, and bupropion
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THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
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Marijuana
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This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic * ileus and urinary retention
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Bethanechol
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Toxicity of organophosphate:
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DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
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Treat manifestations of Parkinson's disease and EPS
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Benztropine, trihexyphenidyl
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Treatment of motion sickness
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Scopolamine, meclizine
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Produce mydriasis and cycloplegia
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Atropine, homatropine,C1208 tropicamide
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Bronchodilation in asthma and COPD
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Ipratropium
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Mnemonic for beta receptors
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You have 1 heart (Beta 1) and 2 lungs (Beta 2)
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This is the drug of choice for anaphylactic shock
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Epinephrine
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These agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
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Alpha1 agonists
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Alpha 1 agonist toxicity
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Hypertension
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Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
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Prazosin, terazosin, doxazosin
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SelectiveB1 Receptor blockers that may be useful in treating patients even though they have asthma
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Acebutolol, atenolol, esmolol, metoprolol
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This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
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Timolol
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These Beta blockers decrease aqueous secretion
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Timolol (nonselective), betaxolol (selective)
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Inhibit peptidyl dipeptidase (plasma kininase)
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ACE inhibitors
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SE of ACE inhibitors
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Cough, hyperkalemia, angioedema
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ACE inhibitors are contraindicated in
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pregnancy and with K+
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Losartan and valsartan block
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Angiotensin AT1 receptor
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Angiotensin receptor blockers do NOT effect
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Bradykinin metabolism
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CCB contraindicated in CHF
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Verapamil
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SE of CCB
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atrioventricular block, constipation, edema
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Agents that reduce heart rate, contractility, and O2 demand
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Beta-blockers
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SE of beta blockers
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Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
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Alpha 1selective blockers
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Prazosin, terazosin and doxazosin (- AZOSIN ending)
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SE of alpha blockers
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Orthostatic hypotension (especially with first dose) and reflex tachycardia
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SE of hydralazine with slow acetylators
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Lupus-like syndrome
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Diuretic used for mountain sickness and glaucoma
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Acetazolamide
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SE of acetazolamide
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Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
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Site of action of loop diuretics
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Thick ascending limb
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SE of loop (furosemide) diuretics
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Hyperuricemia, hypokalemia and ototoxicity
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Loops lose and thiazide diuretics retain
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Calcium
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Site of action of thiazide diuretics
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Work at early distal convoluted tubule
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SE of thiazide (HCTZ) diuretics
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Hyperuricemia, hypokalemia and hyperglycemia
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Potassium sparing diuretics inhibit
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Na+/K+ exchange
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Diuretic used to treat primary aldosteronism
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Spironolactone
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SE of spironolactone
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Gynecomastia, hyperkalemia
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Osmotic diuretic used to treat increased intracranial pressure
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Mannitol
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ADH agonist used for pituitary diabetes insipidus
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Desmopressin (DDAVP)
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MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
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Sodium channel blockers
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SE of procainamide
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Lupus-like syndrome
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Limiting side effect of Quinidine
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Prolongs QT interval
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DOC for management of acute ventricular arrhythmias
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Amiodarone
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Life threatening cardiac event that prolong QT to
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Torsades de pointes
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MOA of sildenafil (Viagra)
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Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
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MOA of nitrates
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Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
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Vitamin K dependent anticoagulant
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Warfarin (PT)
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Heparin (PTT) increases activity of
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Antithrombin 3
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Antidote to reverse actions of heparin
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Protamine sulfate
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SE of Aspirin
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GI bleeding
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MOA of thrombolytics
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Degradation of fibrin clots and are administered IV
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Thrombolytics are used for
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Pulmonary embolism and DVT
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Agent for pernicious anemia
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Cyanocobalamin (Vit B12)
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Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
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Folic acid
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Agent used for anemias associated with renal failure
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Erythropoietin agonists
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MOA of drug or foods (grapefruit juice) that increase statin effect
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Inhibit Cytochrome P450 3A4
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Monitoring parameter to obtain before initiation of STATINS
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LFT's
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Decreases liver triglycerol synthesis
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Niacin
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SE of niacin
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Cutaneous flush
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Fibrates (gemfibrozil) increase activity of
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Lipoprotein lipase
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Agent used for closure of patent ductus arteriosus
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Indomethacin
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Acetaminophen only has
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Antipyretic and analgesic activity
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Antidote for acetaminophen toxicity Drugs-Modifying Anti-Rheumatic Agents (DMARDS)
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N-acetylcysteine
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DMARDs are slow acting drugs for
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Rheumatic disease
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NSAID used in gout
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Indomethacin
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Allopurinol treats chronic gout by decreasing uric acid production by inhibiting
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Xanthine oxidase
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Rapid acting insulins that do not self-aggregate
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lispro insulin, aspart insulin, glulisine insulin
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Peakless long acting insulin
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Insulin glargin
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Diuretic used to antagonize aldosterone receptors |
Spironolactone |
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Selective estrogen receptor modulator used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer |
Raloxifene |
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SE of CCB
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atrioventricular block, constipation, edema
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