Pharm Flashcards
Epinephrine (EPI) acts on what receptors? agonist or antagonist?
α1, α2, β1, β2 agonist
Isoproterenol (ISO) acts on what receptors? agonist or antagonist?
β1, β2 agonist
Norepinephrine (NE) acts on what receptors? agonist or antagonist?
α1, α2, β1 agonist.
phentolamine acts on what receptors? agonist or antagonist?
(α1, α2 antagonist) causes a decrease in systemic vascular resistance (SVR) and reflex tachycardia.
Patients with bulimia or anorexia nervosa should not be prescribed what antidepressant because of the increased risk of seizures?
Bupropion: NE and DA reuptake inhibitor
causes stimulant-like effects such as tachycardia, insomnia, and weight loss.
No sexual activity side effects. Also used in smoking cessation
MOA of chloramphenicol? Major side effect in infants?
inhibits ribosomal peptidyl transferase
“gray baby syndrome”. left untreated, neonates often die of cardiovascular collapse
Fibrates (e.g., gemfibrozil, fenofibrate, and clofibrate) lower triglycerides by approximately 35–50% and increase HDL-c by 5–20%.
MOA?
SE?
Fibrates activate proliferator-activated receptor-α (PPARα) and increase the expression of lipoprotein lipases.
Adverse effects include gallstones and muscle toxicity.
Vecuronium is a nondepolarizing skeletal muscle relaxant that competitively blocks the nicotinic acetylcholine (ACh) receptor.
How do you reverse it’s action in the case of toxicity?
acetylcholinesterase inhibitor such as neostigmine because the increased levels of ACh will compete with vecuronium at the receptor.
Dantrolene MOA and use?
prevents calcium release from the sarcoplasmic reticulum of skeletal muscle by blocking ryanodine receptors.
treat malignant hyperthermia associated with succinylcholine and halothane.
It is also used to treat neuroleptic malignant syndrome
Methimazole is an antithyroid drug similar to propylthiouracil (PTU) used to treat hyperthyroidism,
What is bad side effect?
What should be given if this bad side effect arises?
Agranulocytosis is a potential side effect and occurs in approximately 1:500 patients. Early signs of this complication include fever and sore throat.
Therapy for a patient who develops agranulocytosis is to discontinue the drug and then administer a granulocyte colony-stimulating factor
Cytarabine
MOA, Indication and SEs
antineoplastic used for acute myelogenous leukemia (AML).It is a PYRIMIDINE analog that is commonly administered with idarubicin, daunorubicin or mitoxantrone, to induce remission of acute myelogenous leukemia (AML).
Its mechanism of action is to inhibit DNA polymerase.
Anemia, leukopenia, thrombocytopenia, and megaloblastosis.
Bleomycin
MOA, indication and SE
intercalating agent that complexes iron-forming reactive oxygen species and induces DNA strand breaks.
Used in testicular cancer and hodkin lymphoma
This agent is commonly associated with the development of pulmonary fibrosis (skin hyperpigmentation and minimcal myelosuppression)
Vincristine and Vinblastine
MOA, indication and SE
Vinca alkaloids that bind beta-tubulin and inhibit its polymerization into microtubules –> prevent mitotic spindle formation (M-phase arrest)
Used for solid tumors, leukemias, hodking (vinblastine) and non hodgkin (vincristine) lymphomas
Vincristine causes neurotoxicity (areflexia, peripheral neuritis), constipation (including parlytic ileus)
Warfarin is a vitamin K antagonist necessary for the proper function of clotting factors II, VII, IX, and X.
At clinically relevant doses which factors are effected and what lab values are seen in regards to PT/INR and PTT vs overdose?
At clinical dose only factor VII is affected significantly, resulting in a prolonged PT/INR but a normal PTT.
In warfarin overdose or severe vitamin K deficiency, both PT and PTT are elevated. This effect would also be seen with medication interactions with warfarin such as CYP450 inhibitor
Bleeding time is a functional test of platelet function. Warfarin does not affect platelet count or function so both would be normal
Torticollis may be a side effect of which types of anti-psychotics?
Typical high-potency antipsychotics, such as fluphenazine and haloperidol, are more likely to cause extrapyramidal side effects (EPS).
EPS include acute dystonia, drug-induced parkinsonism, akathisia, and tardive dyskinesia
The drug of choice for localized cutaneous leishmaniasis?
drug of choice for severe diffuse cutaneous and visceral leishmaniasis?
sodium stibogluconate or meglumine antimonate.
Second-line drugs, e.g., amphotericin B and pentamidine, are potentially more toxic, so they are used in the treatment of visceral leishmaniasis cases that are unresponsive to the antimonials.
Amphotericin B is the drug of choice for severe diffuse cutaneous and visceral leishmaniasis.
Pustular acne is treated with which antbiotic and what is its MOA
tetracycline preventing attachment of aminoacyl-tRNA to ribosomes.
Which anticoagulant acts by accelerating the activity of antithrombin III (ATIII) to inactivate thrombin; however, it does not lyse existing clots
Heparin - The aPTT measures the intrinsic system and common pathway, including factors I (fibrinogen), II (prothrombin), V, VIII, IX, X, XI, and XII.
How long does it take a drug to reach steady state? When will it reach 50% steady state, 75%, etc?
It takes four to five half-lives to reach steady-state.
The rule of thumb is that the plasma concentration will reach 50% in one half-life, 75% in two half-lives, 87.5% in three half-lives, etc.
Typical antipsychotics block what receptor to cause most antipsychotic and extrapyamidal side effects?
What specific type of receptor is this and what intracellular events lead to it’s effects?
dopamine 2 (DA2) receptors
Gi which normally will inhibit adenylate cyclase and decrease cAMP production when stimulated.
Blockade of DA2 receptors will, therefore, produce the opposite results and increase cAMP production
What is zileuton? MOA and common indications
5-Lipoxygenase inhibitors such as zileuton act by inhibiting the conversion of arachidonic acid to leukotrienes.
Prevent exercise-induced asthma and can be used to treat chronic asthma in adults and children.
Sirolimus MOA, indication, and side effects?
inhibits T-cell activation and proliferation by binding mTOR
indicated for kidney transplant rejection prophylaxis
sometimes severe worsening of preexisting hypercholesterolemia and hypertriglyceridemia.
Other serious adverse effects associated with sirolimus include atrial fibrillation, heart failure, hypervolemia, and palpitations.
Drug of choice for fungal toenail infections?
Terbinafine
What do Trihexyphenidyl and Amytripyline have in common?
Antimuscarinic side effects
When graphing drug effect vs concentration how will administration of a competitive antagonist vs a noncompetative antagonist change the shape of an agonist?
Competitive=Change ED50=shift right (no change in max effect)
Noncompetitive=Change Emax=shift down
Why should you worry about giving Linezolid with an SSRI?
Linezolid has MAOI activity and can precipitate serotonin syndrome
Triad: autonomic instability (hyperthermia, hypertension, tachycardia), AMS (agitation and confusion) and neuromuscular hyperactivity (tremor, hyperreflexia, and myoclonus)
what are the two classes of dopamine agonists?
Ergot compounds (bromocriptine) and nonergot compounds (pramipexole and ropinerole)
MOA of class III antiarrhytmic drugs (amiodarome, sotalol, and dofetilide)
predominantly block potassium channels and inhibit the outward potassium currents during phase 3 of the cardiac action potential, thereby prolonging repolarization and total action potential duration.
Class IA antiarrhythmic drugs. What are they and MOA?
Quinidine, procainamide, and disopyramide
predominantly inhibit sodium dependent (phase 0) depolarization and slow conduction. They also have moderate potassium channel blocking activity, leading to prolonged action potential duration.
Side effects of Niacin?
flushing, hyperglycemia, hepatotoxicity, and decreased renal excretion of uric acid –> increased risk for gouty arthritis
What accounts for quick onset and short duration of propofol and other drugs like it?
Propofol is highly lipophilic so can be rapidly cleared from the plasma and preferentially distributed to organs receiving high blood flow (brain). over time redistributed to organs with less blood flow (muscle and fat)
How do nitrates work (step by step explanation)
nitrates (conversion to nitric oxide) activate guanylate cyclase and increase intracellular levels of cyclic guanosine monophosphate (cGMP). Increased levels of cGMP lead to myosin light-chain dephosphorylation, resulting in vascular smooth muscle relaxation.
Antibiotic of choice for treating lung abcesses of alcoholics (anaerobic oral flora and aerobic bacteria)
Clindamycin covers most of these organisms and is thus the antibiotic of choice for treating lung abcesses
Niacin is used to tx hyperlipidemia because it increases HDL and decreases LDL and triglycerides. The side effect of flushing is mediated by what and can be diminished by pre-treating with what?
Mediated by prostaglandins
pre-treat with aspirin
Advantage of buspirone over benzo’s in treating anxiety is?
no risks of tolerance, dependence, or withdrawal
has no muscle relaxant or anticonvulsant properties. fewer sedative and hypnotic effects and does not cause euphoria
How does pernicious anemia effect gastrin secretion and intraluminal pH?
autoimmune disease results in destruction of parietal cells (decreased secretion of intrinsic factor results in B12 deficiency and megaloblastic anemia)
with parietal cell destruction there is decreased H+ secreted resulting in increased pH and increased secretion of gastrin
What drug is used to treat malignant hyperthermia and what is it’s MOA?
Dantrolene
blocks ryanodine receptors and prevents release of Ca into the cytoplasm of skeletal muscle fibers.
How do direct factor Xa inhibitors (apixaban and rivaroxaban) effect PT, PTT, and TT?
prolong aPTT and PT but no effect on TT
