Pharm 1 Flashcards
What is Varenicline used for and how does it work?
It is a partial agonist for nicotinic ACh receptors and assists pts with cessation of tobacco use by reducing withdrawal cravings and attenuating reward effects of nicotine
What is topiramate used for?
It is an anticonvulsant used to treat epilepsy in children and adults and it is an effective med for migraine prophylaxis
MOA of Caspofungin and other echinocandin antifungals
block 1,3-beta-D-glucan synthesis in fungal cell wall
-most active against Candida and Aspergillus
MOA of Amphotericin B
polyene antifungal that binds ergosteral in the fungal cell membrane and leads to pore formation and cell lysis
MOA of itraconAZOLE
azoles are antifungals that inhibit ergosterol synthesis
MOA of Terbinafine
inhibits the fungal enzyme squalene-2,3-epoxidase which results in decreased synthesis of ergosterol
-this accumulates in skin and nails and is used to treat dermatophytosis
MOA of Griseofulvin
binds microtubules and inhibits mitosis
-effective only against dermatophyte fungi and accumulates in keratin containing tissue
MOA of Flucytosine
inhibits synthesis of DNA and RNA in fungal cells
-synergistic with amphotericin B in Tx of cyrptococcal meningitis
What kind of antiarrhythmic is Dofetilide?
Class 3 antiarrhythmic that blocks K+ efflux from cardiac myocyte and prolongs phase 3 of the myocyte AP
What is the most common cause of macrovesicular fatty change?
chronic ethanol consumption
What is a common cause of microvasicular fatty change in children?
Reye syndrome
What is a major side effect of halogenatied inhalation anesthetics and which drug is the most common cause?
Halogenated inhalation anesthetics can cause massive hepatic necrosis d/t direct liver injury and autoantibodies against liver
-halothane is the most common
What drugs are structural analogs of D-Ala-D-Ala that inhibit transpeptidase?
Penicillins
What is the term when when a drug needs to be given at a larger dose to achieve the same clinical effect previously achieved with a smaller dose?
Tolerance
What is the AE of using nitrates with PDE inhibitors?
They both increase intracellular cGMP which causes vascular smooth muscle relaxation and hypotension
What occurs with stimulation of a1 adrenoreceptors?
vasoconstriction in skin and viscera resulting in increased SBP and DBP with decreased renal and hepatic blood flow
Side effects of this antiarrhythmic include thyroid dysfunction, lung fibrosis, liver toxicity, and blue/grey discoloration of skin
amiodarone
Side effects of this antiarrhythmic include nonfocal neurologic signs such as tremor, drowsiness, change in mental status, and generalized seizure
lidocaine
Side effect of this antiarrhythmic include negative inotropy, constipation, and gingival hyperplasia
verapamil
This drug is used as a vasodilator in chemical cardiac stress tests and as a fast acting antiarrhythmic for stopping acute supraventricular tachycardias
Amiodarone
If a pt has lupus-like Sx (erythematous rash on face and trunk, joint pain, photosensitivity) and + ANA and anti-histone, what are the common drug-induced lupus associations?
HIPP hydralazine isoniazid procainamide phenytoin
How does Ezetimibe decrease serum LDL?
decrease intestinal absorption of dietary cholesterol
What is the antidote for tissue necrosis d/t NE infusion through an IV site?
local injection of an alpha1 blocker like phentolamine
What is an example of a poorly soluble gas anesthetic and what are its effects?
N2O
- small amount needed to saturate blood
- low blood/gas partition coefficient
- rapid rise in partial pressure in blood
- rapid equlilbration with brain
- rapid onset
What is an example of a highly soluble gas anesthetic and what are its effects?
halothane
- large amount needed to saturate blood
- high blood/gas partition coefficient
- slow rise in partial pressure in blood
- slow equilibration with brain
- slow onset
What are the properties of drugs with high blood/gas partition coefficients?
more soluble in blood, slower equilibration with brain, longer onset time
What are the properties of drugs wtih low blood/gas parititient coefficients?
less soluble in blood, faster equilibration with brain, shorter onset time
What antidepressant class is particularly useful in pts with atypical depression and treatment-resistant depression?
monoamine oxidase - phenelzine and tranylcypromine
What are the characteristics of atypical depression?
mood reactivity
leaden fatigue (arms and legs feel heavy)
rejection sensitivity
increased sleep and appetite
What is the main characteristic of atypical depression that distinguishes it from major depression?
mood reactivity
-atypical depression pts will improve mood in response to something psotive, typical major depression pts will not have a change in mood
What is the MOA of sucralafate?
It binds to the base of gastric mucosal ulcers and provides physical protection against acid
What is the MOA of bethanecol?
it is a cholinomimetic muscarinic agonist that treats urinary retention and ileus
What class of drugs block the final common pathway of gastric acid secretion of parietal cells that is stimulated by ACh, histamine, and gastrin?
PPIs
What is the MOA of cimetidine?
blocks the gastric parietal cell histamine H2 receptor
What is the MOA of probenecid?
decreases proximal tubular uric acid reabsorption, often used to lower serum uric acid levels in CHRONIC gout
What is the MOA of allopurinol?
inhibition of xanthine oxidase which lowers serum uric acid levels in CHRONIC gout
what drug is indicated for acute gouty arthritis and what is the MOA?
Colchicine - inhibits tubulin polymerization and microtubule formation in leukocytes which reduces neutrophil chemotaxis and migration to sites inflamed by uric acid deposition
What are AE of colchicine?
diarrhea, N/V bc GI mucosa is adversely affected
When do you most often see hyperkalemia associated with ACEi?
ACEi induced hyperkalemia is most common in pts with renal insufficiency and pts taking K+ sparing diuretics such as amiloride, triamterene, spironolactone, and eplerenone ore K+ supplements
What are the two types of K+ sparing diuretics?
ENaC blockers: amiloride and triamterene
aldosterone antagonists: spironolactone and eplerenone
What is the MOA of verapamil?
CCB - blocks Ca2+ channels in vascular smooth muscle and myocardium and leads to vasodilation and reduced oxygen demands
What are 3 common SE of verapamil?
constipation, peripheral edema, and bradycardia
What is the MOA of indapamide and hydrochlorothiazide?
thiazide diruretics that block Na+/C;- symporters in distal tubules
What is the MOA of Amlodipine?
CCB that only blocks vascular smooth muscle that results in peripheral vasodilation and improved coronary blood flow; can cause reflex tachycardia
What is a Hx of “mood swings” suggestive of?
bipolar disorder
When are carbamazepine, lithium, and valproate appropriate therapies for mental disorders?
they are mood stabilizers used in acute mania and maintenance Tx of bipolar disorder
What is important to monitor on lithium therapy?
lithium blood levels, periodic assessment of TSH, AND RENAL bun FUNCTION
What are SE of carbamazepine and valproate?
anticonvulsants associated wtih risk of liver enzymes and NTDs
What is Olanzapine and what is a SE?
2nd generation antipsychotic with mood-stabilizing properties used in bipolar disorder
SE: weight gain and metabolic SE
What is an anticonvulsant mood stabilizer effective in the depressed phase of bipolar disorder and associated with rash and SJ syndrome?
Lamotrigine
What MOA of Venlafaxine and when should it be used with caution?
SSRi antidepressant - risk of inducing mania in susceptible pts, esp with unrecognized bipolar disorder
What lipid lowering agent inhibits lipolysis in adipose tissue and reduces hepatic VLDL secretion into circulation? What are the SE?
Niacin (increase nice cholesterol)
SE: red flushed face, hyperglycemia, hyperuricemia
What lipid lowering agent prevents intestinal reabsorption of bile acids so that liver must use cholesterol to make more? What are the SE?
bile acid resins: cholestyramine, colestipol, colesevlam (decrease bad cholesterol and binds bile in GI tract)
SE: tastes gross, GI discomfort, decreased absorption of DEKA, cholesterol gallstones
What lipid lowering agent prevents cholesterol reabsorption at the small intestine brush border? What are the SE?
cholesterol absorption blockers: ezetimibe
SE: rare increase in LFTs, diarrhea
What lipid lowering agent upregulates LPL and increases TG clearance? What are the SE?
fibrates: gemfibrozil, clfibrate, bezafibrate, fenofibrate
SE: myositis, hepatotoxicity, cholesterol gallstonesq
What are the effects of statins and bile acid resins on cholesterol production? What is the effect of combo therapy?
simvastatins decrease and cholestyramine increase hepatic cholesterol production
combo therapy results in net decrease in hepatic holesterol synthesis and plasma LDL level
which lipid lowering agents increase the risk of gallstones?
agents that increase hepatic cholesterol synthesis: fibrates and bile acid-binding agents
What drug can cause epinephrine to paradoxically increase insulin secretion
Phenoxygenzamine: long-acting nonselective alpha blocker. Since Epi can bind to both a and B recetors on pancreas, blockage of alpha-receptors allows more Epi to bind B receptors and results in increased insulin secretion
What is the most common side effect of ethambutol used for TB?
optic neuritis - manifests as decreased visual acuity, central cotoma, or color-blindness
What 3 antibiotics should you monitor CBC for?
Chloramphenicol: aplastic anemia
TMP-SMX: megaloblastic anemia
Dapsone: agranulocytosis
Which TB drug requires an acidic environment (within macropahge phagolusosomes) to kill TB?
Pyrazinamide
What patient population is most likely to develop pulmonary infections and abscesses involving combos of anaerobic oral flora (Bacteroides, Prevotella, Fusobacterium, and Peptostreptococcus) and aerobic bacteria and what is the antibiotic of choice?
Alcoholics - Tx with Clindamycin
What are the effects of adding carbidopa to L-dopa therapy?
adding carbidopa inhibits the peripheral conversion of levodopa, making it more available to the brain
why are nausea and vomiting Sx reduced with L-dopa + carbidopa therapy? What other peripheral Sx are reduced?
still considered peripheral, because located outside the BBB
-other peripheral Sx: tachyarrhythmias, hot flashes, and postural hypotension
What side effect is still seen and may be enhanced with L-dopa + carbidopa therapy?
behavioral changes such as anxiety and agitation may still be seen because more DA is available to the brain
Ventricular myocyte depolarization mediated by inward Na+ movement is modulated by what class of antiarrhythmics?
class I antiarrhythmics
what does the QRS complex correspond to?
ventricular depolarization and phase 0 on the action potential graph
What is the most common side effect of Phenelzine?
Phenelzine is a MAO inhibitor that may lead to severe hypertensive crisis with tyramine-containing foods, such as cheese, sausage and wine.
Why do MAO inhibitors lead to hypertensive crisis?
they block degradation of amine NTs such as NE which accumulate in presynaptic stores
What is the MOA of SSRIs?
these are presynaptic selective serotonin reuptake inhibitors: fluoxetine, sertraline, and paroxetine which block reuptake of serotonin at pre-synaptic neuron so more serotonin accumulates within the synaptic cleft to counteract depressive Sx
What is the MOA of bupropion?
Bupropion is a presynaptic selective NE uptake inhibitor - associated with agitation, insomnia, and seizures
What is the MOA of TCAs?
presynaptic non-selective monoamine uptake - imipramine, amitriptyline, and clomipramine
-these block the amine (NE or serotonin) reuptake pumps which terminate amine transmission - this permits tehse amines to remain for longer time periods at the receptor site
What is hyperpyrexia and what are common triggers?
body temperature greater than 40 C
triggers: severe infection, malignant hyperthermia, neurolepitc malignant syndrome, heat stroke
First line Tx: cool pt - cool blankets
What is necessary for a pt with hyperthyroidism receiving methimazole or PT presenting with a fever and why?
WBC count with differential to look for agranulocytosis
What is the most feared SE for antithyroid drugs PTU and methimazole?
agranylocytosis (neutrophil count <500/mL)
What is the antidote of choice in a heroine OD and why is it effective?
Methadone - mu receptor agonist that is a potent, long acting opiate with good oral availability
-its LONG HALF-LIFE leads to continuous suppression of withdrawal Sx
What is ST elevation in inferior leads diagnostic of?
inferior MI - blockage of RCA which is responsible for SA and AV perfusion - will show bradycardia
What is the antidote for bradycardia d/t inferior MI and what is a side effect?
Atropine - blocks vagal influence of SA and AV node via mAChR and can also lead to mydriasis resulting in narrowing of anterior chamber angle and precipitate angle-closure glaucoma
What are 3 beta-lactamase inhibitors?
calvulanic acid, sulbactam, and tazobactam
What can be used to treat male-pattern baldness?
5-a-reductase inhibitors like finasteride
How does N-acetylcysteine work as a Tx of CF?
It is a mucolytic agent that cleaves disulfide bonds within mucus glycoproteins, thus loosening thick sputum
What is the MOA of misoprostal?
PGE1 analog used to prevent NSAID-induced ulcer disease
What is the best way to provide long-term relief for PUD pts?
Eradicate H. pylori with antibiotics : combine 2 antibiotics (metronidazole, tetracycline, amoxicillin, or clarithromycin) with an adjunctive agent (PPIs and/or bismuth) for 14 days
What is an agent you can give for urge incontinence/detrusor instability?
antimuscarinic (M3) drug such as oxybtynin
What is Risperidone used for and what are its side effects?
anti-psychotic used for schizophrenia
SE: hyperprolactinemia –> amenorrhea, galactorrhea, and breast soreness
