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185 Cards in this Set
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Botulinum Toxin A (Botox)
mechanism of action? |
prevents the release of ACh by cleaving the vesicular fusion apparatus SNAP-2
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how it prevents the release of ACH?
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Baclofen mechanism of action?
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Binds and activates GABAb to reduce tonal neural stimulation to muscles.
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it is a muscle relaxant
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Indications for Baclofen?
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a spasmolytic for patients with multiple sclerosis or spinal cord lesions
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its mechanism of action is to bind and activate inhibitory GABAb channels in the CNS
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Dantrolene mechanism of action
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A muscle relaxant that works by blocking calcium release from the SER to reduce skeletal muscle contraction
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it isu sed in the treatment of malignant hyperthermia
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Dantrolene - indications
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treatment of malignant hyperthermia or neuroleptic malignant syndrome
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its mechanism of action is to block the release of calcium from the SER of skeletal muscles.
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Minoxidil
mechanism of action |
it is an arterial vasodilator used as an adjuct for hypertension but more useful for its side effect of hair growth (Rogaine)
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effects on smooth muscle cells
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Minoxidil - effect on the pancreatic beta cells
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it causes a decrease in insulin response to glucose = hyperglycemia?
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this is also known as rogaine and has an antihypertensive effect
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Atenolol - mechanism of action
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selective B-1 blocker
it reduces contractility and heart rate it causes reduced renin secretion |
selective or non selective? how does it work as an antihypertensive?
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Clonidine - Class
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alpha-2 agonist
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acts to reduce sympathetic tone by down regulating NE release (presynaptic). Also vasoconstricts (postsynaptically)
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Clonidine - Indications (2)
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Hypertension and treatment of opioid withdrawal
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Even though it acts as a vasoconstrictor on postsynaptic cells, the predominant action of lowering sympathetic tone allows it to work as this.
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Losartan - class
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ARB
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good to use when someone cannot tolerate an ACEi
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Phentolamine
Mechanism of Action |
nonslective alpha-blocker
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used to control pheochromocytoma
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Name two drugs that are ideal treatment for pheochromocytoma
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phentolamine and phenoxybenzamine
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they are alpha blockers
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5-FU
Mechanism of Action |
antimetabolite that inhibits thymidylate synthetase
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5-FU
Major Side Effects (2) |
bone marrow suppression
GI mucositis |
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5-FU
Indications |
solid tumors (i.e. colon, breast) and topical for some skin issues
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Acetaminophen
Treatment of Overdose |
N-acetylcysteine
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causes liver toxicity in high doses
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Acetazolamide
Class |
Diuretic: Carbonic Anhydrase Inhibitor
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acts on the PCT
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Carbonic Anhydrase inhibitors
Site of Action |
PCT
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Acetazolamide
Indications |
alkalosis (Alkalinization of urine)
glaucoma (decr. aqueous humor) high altitude sickness |
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Which (2) classes of antiarrhythmics are contraindicated in long QT syndrome?
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Class IA and III.
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Antiarrhythmic that is used for diagnostic and theraputic purposes for SVTs and also for pharm. cardiac stress tests.
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Adenosine
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Mechanism of action of class III antiarrhthmics.
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Potassium channel blocker (prolongs repolarization)
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Amiodarone
Class |
Class III
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Amiodarone
Side Effects (4) |
pulmonary fibrosis
increases QT interval thyroid dysfunction sometimes liver dysfunction |
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Flecanide
Class |
Antiarrhthmic class IC (potent sodium channel blockers)
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Mechanism of Action
Antiarrhthmics Class IC |
potent sodium channel blockers
decrease slope of phase 4 and raise threshold |
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Metoprolol
Class of antiarrhythmic |
Class II
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Flecanide
Indications |
only to be used on people with structurally normal hearts ("flec and die") with SVT
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Verapamil
Antiarrhythmic class |
Class IV (Calcium Channel Blockers)
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Zileuton
Mechanism of Action |
inhibits 5-lipoxygenase
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Name the drug that is a prostacyclin used to treat pulmonary hypertension. It acts by stimulating PGI2 receptors
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Epoprostenol
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Misoprostol
Indications (2) |
ulcers
miscarriages |
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Misoprostol
Mechanism of Action |
agonist of PGE1
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Zarfirlukast
Mechanism of Action |
blocks leukotriene receptors (LTD4)
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monteluklast
Mechanism of Action |
leukotriene antagonist
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Alprostadil
Indications (2) |
impotency
maintain ductus arteriosis |
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Alprostadil
Mechanism of Action |
Agonist of PGE1
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Dinoprostone
Indication |
softening/ripening of cervix and induction of labor
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Dinoprostone
Mechanism of Action |
PGE2 agonist (oxytocin agonist)
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Glyburide and glipizide are what class?
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sulfonylureas
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Mechanism of action of sulfonylureas?
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Secretogogues - stimulate pancreatic beta cells to release insulin. Also may help insulin bind to its receptor and/or increase the number of receptors.
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Which organ clears sulfonylureas (glyburide and glipizide)?
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The liver. Thus do not use in folks with liver issues. Is a good choice in folks with renal issues.
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Which class is metformin?
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Biguanide
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Mechanism of action of metformin? (2)
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decreases liver gluconeogenesis and increases tissue glucose uptake
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Major side effect of metformin? Who is at most risk?
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Lactic acidosis - increase risk of this in those with heart disease or renal failure
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Class: Rosiglitazone, pioglitazone
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Thiazolidinediones
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Mechanism of action of Thiazolindinediones?
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Bind PPAR-gamma receptor to increase tissue sensitivity to insulin (increase glucose uptake) and inhibit liver from making more glucose
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Side effect of Thiazolidinediones
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Liver toxicity (think about how it inhibits the liver from making more glucose)
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Acarbose and miglitol are what class?
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Alpha-glucosidase inhibitors
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Mechanism of action of alpha-glucosidase inhibitors (acarbose and miglitol)
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Inhibition of the enzyme decrease glucose absorption in the GI tract.
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Useful in the treatment of carcinoid syndrome since it inhibits release of tumor hormones and aids the symptoms of flushing and diarrhea.
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Octreotide (somatostatin analogue)
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Serotonin (5-HT3) blocker used for diarrhea predominant IBS?
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Alosetron
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Orally active cannibanoid that is used as an antiemetic in chemotherapy?
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Dronabinol
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Class of Famotidine
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H2-blocker
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Class: Lansoprazole
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PPI
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An amphetamine derivitive used to decrease appetite
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Phentermine
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Sulfasalazine is an anti-inflammatory used in the treatment of what?
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Ulcerative colitis.
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What is ursodiol used for?
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to break up gallstones.
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Theophylline
Drug-drug interactions? |
theophylline is extensively metabolized by the liver P450 enzyme system so be careful not to mix with enzyme inhibitors like erythromycin.
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Which macrolide is a potent inhibitor of the P450 enzyme system so must be used with caution in patients on meds like Warfarin or Theophylline?
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Erythromycin
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Mycoplasma, which have no cell wall, are inherently resistant to this drug.
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Amoxicillen - because it has an amino group that makes it hydrophilic so it can cross cell walls of G(-) bugs
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This second-generation cephalosporin is associated with serum sickness.
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Cefaclor
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Gray baby syndrome
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chloramphenicol
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Which electrolyte may get dangerously high in the treatment of hypertension with an ACEi such as enalapril?
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Potassium. You get hyperkalemia because you don't have as much aldosterone made therefore the kidney is not stimulated to pee out all of the K.
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This drug is used in the tx of AML. Its MA is to inhibit DNA polymerase. Its ADE are leukopenia and anemia.
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Cytarabine.
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MOA of Bleomycin
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intercalates DNA
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Mechanism of Action of Doxorubicin.
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breaks DNA, intercalates DNA, oxidizes free radicals
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Topoisomerase inhibitor used for the treatment of testicular cancer, small cell lung cancer, and leukemia.
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etoposide
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Mechanism of action of Paclitaxil
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Binds tubulin and prevents it from depolymerizing.
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Mechanism of Action of Ticlopinide
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inhibits ADP-induced platelet aggregation
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Mechanism of Action of the chemotheraputic agent mycophenolate mofetil?
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inhibits de novo synthesis of purine (Guanine)
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Which immunosuppressant drug has the mechanism of action of inhibiting calcineurin-mediated transcription of IL-2?
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tacrolimus or cyclosporine (they have the same mechanisms)
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Which migraine medication has the rare but deadly side effect of malignant HTN?
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sumatriptan (Imitrex)
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Diclofenac - class?
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NSAID
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Ergotamine - Mechanism of Action?
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Vasoconstrictor used to treat migraines. It acts on multiple receptors. Contraindicated in preggers or CAD pts.
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Class - Methylsergide
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anti-migraine
seratonin antagonist and weak vasoconstrictor |
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Mechanism of Action
Sumatriptan |
5-HT d1 agonist
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Mechanism of Action
Chlorambucil |
DNA alkylating agent (nitrogen mustard)
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The primary (2) indications for use of chlorambucil are
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CLL and ovarian cancer
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Mechanism of Action
Cisplatin |
cross-links DNA (alkylating)
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Mechanism of Action
Vinblastine |
depolymerizes microtubles
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Main Indication for Vinblastine
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Hodgkins
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Main side effect of vinblastine
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peripheral neuritis
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Immunosuppressive agent used esp. in kidneys that works as a purine antagonist and is metabolized by xanthine oxidase
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azathioprine - so take care if you give allopurinol, an inhibitor of xanthine oxidase, because you can get azathioprine toxicity (myelosuppression)
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Treatment of Wilson's disease
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penicillamine
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Clonidine - class
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alpha-2 receptor AGONIST
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What action do alpha-2 receptors have on pancreatic beta cells?
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directly inhibit insulin secretion
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Class - terbutaline
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beta-2 agonist
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What action do beta-2 agonists have on pancreatic beta cells?
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stimulate the release of insulin
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Why do patients on digoxen therapy often develop arrhythmias? Hint - concurrent meds.
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Diruetics such as furosemide that cause them to become hypokalemic or mypomagnesismic.
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What is colestipol?
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A bile acid binding resin that is used for hypercholesterolemia.
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Effect of drugs with sulfa components on digoxin?
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Lower digoxin levels
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Effect of phenytoin on digoxin
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lowers its levels
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effect of sulfasalazine on digoxin?
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lowers its levels (remember all sulfa components do this).
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Site of Action of potassium sparing diuretics
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collucting duct
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class - ethacrynic acid
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loop diuretic
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mechanism of action and site of action of loop diuretics
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inhibit the Na K Cl cotransporter
thick ascending loop of henle |
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site of action of thiazide diuretics
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DCT
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mechanism of action of thiazide diuretics
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inhibit the action of the Na Cl pump in the DCT
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Treatment of choice for pneumonia caused by strep pneumo
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penicillin G
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Ceftazidine (3rd gen ceph) is effective against
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psuedomonas and gram negatives, not really good for gram positives even compared to other 3rd genners
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class - ciprofloxacin
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fluoroquinolone
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Is cipro, a fluoroquinolone, effective against strep pneumo?
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no - although it does have gram negative activity
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can you use macrolides or TMP-SMX to treat CAP?
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no - there are high numbers of resistant orgs of strep pneumo
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class of drugs that binds reversibly to 50S ribosome
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macrolides
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Tizanadine
Mechanism of Action |
alpha 2 agonist (like clonidine) - is used as a centrally-acting muscle relaxant
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Tizanadine
Indications |
Muscle relaxant used for muscle spasms from spinal cord injury, MS, cerebral palsy, stroke, etc. It acts as an alpha-2 agonist like clonidine.
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Name a drug used to increase appetite
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Megestrol (Megace)
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Loperimide
Indications |
OTC antidiarrheal
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Ondansetron
Class/Mechanism of action |
anti-emetic
5-HT3 (serotonin) blocker |
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Sibutramine
Class |
MAO inhibitor (decreases appetite because it reuptakes serotonin)
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Which class of antibiotics, when taken with antacids, has its bioavailability drastically reduced?
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fluorquinolones
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Name as many drug classes as you can that are known to cause AIN (7)
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NSADS
beta-lactam antibiotics diuretics phenytoin cimetidine methyldopa |
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Name the side effects of loop diuretics
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ototoxicity
hypokalemia metabolic alkalosis hyperglycemia *the reduced sodium stimulates the renin-angiotensin-aldosterone axis |
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Which class of antibiotics should be avoided in people with MG and why?
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aminoglycosides have some antinicotinic (curare-like) effects.
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mechanism of action of aminoglycosides
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clock formation of initiation complex by binding the 30S subunit of bacterial ribosomes
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class: gentamycin
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aminoglycoside
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class - neomycin
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aminoglycoside
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class: tobramycin
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aminoglycoside
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class: streptomycin
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aminoglycoside
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aminoglycosides are effective against
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gram negatives.
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OD on which drug would cause tachycardia, elevated body temperature, mydriasis, and skeletal muscle weakness?
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botulinum toxin - note that many other drugs would cause all of these symptoms except for the muscle weakness (due to lack of ACh on NMJ sites)
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Doxepin is indicated for the treatment of
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depression
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Two common side effects of the TCA doxepin are
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anticholinergic effects of dry mouth and tachycardia (it blcks muscarinics)
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Once a head CT reveals no hemmorhage, you can treat a cerebral stroke with
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tPA
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What is the mechanism by which estrogen replacement helps osteoporosis?
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it inhibits osteoclastic activity and aids in osteoblastic activity
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Treatment of tinea corporis?
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antifungals: clotrimazole cream (miconazole or econazole also work)
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Describe what contraction alkalosis is as a side effect of loop diuretic therapy.
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Loop diuretics cause lots of salt and water to be lost from the ECF which in turn causes an increase in the relative bicarb concentration.
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Mechanism of action of thiazolidinediones
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increase insulin sensitivity and therefore have a moa most similar to that of diet and exercise
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Which antiarrhythmic drug (class) acts by decreasing SA node automaticity, increasing AV node refractiveness, and decreasing AV nodal conduction velocity
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propanolol (class II antiarrhythmic
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Mechanism of Action
Amiodarone |
Class III antiarrhythmic
prolongs action potential duration |
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Disopyramide
class |
Ia antiarrhythmic
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Mechanism of Action
Disopyramide |
sodium channel blocker
reduces phase 0 depolarization' increases action potential duration |
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Lidocaine
class |
IB antiarrhythmic
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Mechanism of Action
Chloramphenicol |
inhibits ribosomal peptidyl transferase
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Although it is no longer used much in the USA because of the risk of aplastic anemia, chloramphenicol was indicated for
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typhoid fever and salmonella
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Mechanism of Action of Phenytoin
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Class IB antiarrhythmic - blocks sodium channels
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Tocainide
Class |
Class IB antiarrhthmic
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Mechanism of Action
Digoxin |
increases cardiac contractility by acting on the K/Na ATPase on cell membranes
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Sotalol
Class |
Class III antiarrhthmic
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Mechanism of Action
acyclovir |
inhibits viral DNA polymerase
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Symptoms of OD of Jimson Weed
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an anticholinergic
dry as a bone, red as a beet, mad as a hatter, hot as hades, inactive BS, tachycardia |
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Which two medications are most commonly used to treat Chlamydia?
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Azithromycin or doxycycline
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Cisplatin and cyclophosphamide, isofosphamide are what level emetics?
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level 5 - bad
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decarbazine is what level emetic?
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level 5
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Bleomycin and Vincristine are what level entiemetics?
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level 1
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mercaptupurine is what level antiemetic?
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level 1 -good
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What are the side effects of cyclobenzaprine?
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anticholinergic effects such as dry mouth. It is a centrally acting muscle relaxant structurally related to TCAs.
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Which neurotransmitter is important in the induction of REM sleep?
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ACh
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Mechanism of Action
Vincristine |
blocks the formation of microtubules
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Mechanism of Action
Paclitaxil |
prevents the depolymerization of microtubules
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Mechanism of Action
Doxirubicin |
inserts between DNA to cause strand breakage
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Mechanism of Action
Bleomycin |
intercalates DNA, causing strand breakage
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Which class of diabetic drugs works by decreasing hepatic gluconeogenesis and increase muscle glucose uptake?
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thiazolidinediones
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chlorpropamide
class |
sulfonylurea derivative that stimulates insulin secretion from the pancreas
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glyburide
class |
sulfonylurea derivative that stimulates insulin secretion from the pancreas
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mechanism of action
miglitol |
decreases absorption of glucose in the GI tract
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tolbutamide
class |
sulfonylurea derivative that stimulates insulin secretion from the pancreas
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How can you tell apart the amides from the esters of local anesthetics?
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amides have two i's and esters have one i
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where are local anesthetic amides metabolized?
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liver
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where are local anesthetic esters metabolized?
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plasma cholinesterases
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mechanism of action of local anesthetics
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block voltage-gated sodium channels from the inside
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how can you increase the duratino of action of a local anesthetic?
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administer it with a vasoconstrictor such as epi in order to reduce blood flow
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Lidocaine, an amide local anesthetic, is also
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class IB antiarrhythmic
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mode of use of benzocaine
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topical only
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which local anesthetic is most notable for CV toxicity as a side effect?
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benzocaine
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Which immunosuppressant drug has the mechanism of action of being a monoclonal antibody directed at the IL-2 receptor on activated T cells?
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daclizumab
(also basiliximab) |
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Merperdine
class |
Opioid agonist
drug of choice with acute cholecystitis because it is least likely to cause spasm of sphincter of oddi |
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Drug of choice for myoclonic jerking syndromes - because it is very effective and non-sedating
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valproic acid
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Enzyme that activates mercaptopurine?
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HGPRT
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Main ADE of mercaptopurine
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hyperuricemia (avoid allopurinol in this special case because it inhibits the enzyme that metabolizes this drug) and myelosuppression
hepatotoxicity with long term use |
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anastrozole
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estrogen antagonist used to treat breast cancer
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the anticholinergic side effects of TCAs such as amitryptiline can have this sever outcome
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attack of acute angle glaucoma (blocked muscarinic receptors on constrictor puppilae muscel result in dilation which narrows the angle)
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Cimetidine
class |
H2 blocker
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malothion
class |
organophosphate
cholinesterase inhibitor (increases ACh levels) used as pesticide |
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Treatment of HCM
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beta blockers
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Antibiotic that has serum sickness as a side effect more prominently in children than adults
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cefaclor
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Treatment of serum sickness caused by cefaclor
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prednisone and benadryl
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sodium stibogluconate and meglumine antimonate are used to treat
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leshmaniasis
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Side effects of sirolimus
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HYPERLIPIDEMIA
avoid high fat meals (thrombocytopenia and leukopenia) |
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Sirolimus
Mechanism of action |
inhibits T-cell proliferation
(binds mTOR, a serine-threonine kinase crucial for cell replication) |
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major side effect
muromonab CD3 |
cytokine release syndrome
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cyclosporine and tacrolimus are limited by
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nephrotoxicity
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Treatment of HIT
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bivalirudin or lepirudin (these are direct thrombin inhibitors) (protamin is not enough for HIT)
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