Deja Review pharm Flashcards
volume of blood cleared of the drug per time
Clearance
rate of elimination/plasma concentration
Calculation for half life
t1/2= (0.7 x Vd) / Cl
Calculation for loading dose
Loading dose= (Vd x steady state concentration) / F (bioavailability)
Calculation for maintenance dose
(Cl x steady state concentration x dosing interval) / F
What happens to the loading dose in patients with hepatic or renal failure?
Stays the same
What happens to the maintenance dose in patients with hepatic or renal failure?
Decrease
Constant rate of elimination regardless of concentration is characteristic of
Zero order elimination
Rate of elimination proportional to concentration is characteristic of
First order elimination
Stage of drug trial where you look for safety in a small group of healthy individuals
Phase 1
Stage of drug trial where you look for efficacy in diseased individuals in small scale trials which can be single or double blind
Phase 2
Stage of drug trial where you look for efficacy in diseased individuals in large scale double blind trials
Phase 3
Stage of drug trial undergoing post-marketing surveillance
Phase 4
2 Agents used to acidify urine
NH4Cl and high dose vitamin C
2 agents used to alkalinize urine
NaHCO3 and acetazolamide
Inducers of p450
phenobarbital (barbituates), rifampin, phenytoin, carbamazepine, St. John’s wort, chronic ethanol inoxication
Inhibitors of p450
Erythromycin, ketoconazole, quinidine, cimetidine, chloramphenicol, grapefruit, Acute ethanol intoxication
Intracellular volume makes up what fraction of TBW
2/3
Extracellular volume makes up what fraction of TBW
1/3
Interstitial volume makes up what fraction of extracellular volume?
2/3
Plasma volume makes up what fraction of the extracellular volume
1/3
A competitive antagonist does what to the potency and maximal response of the agonist?
Decreases potency and does not change maximal response (causes a parallel right shift in dose/response curve)
A noncompetitive antagonist does this to the potency and maximal response of the agonist?
Potency does not change
maximal response decreases (causes a non-parallel shift to the right on dose/response curve)
give 2 drugs that are examples of potentiators
Benzos and barbituates potentiate the effect of GABA on its receptor
How do you calculate therapeutic index?
LD50/ED50
High yield drugs to be aware of with a narrow therapeutic index
Warfarin, digoxin, lithium, phenytoin, valproic acid, theophylline, carbamazepine, levothyroxine
Bacteria that become resistant to vancomycin change their D-ala D-ala terminus to what?
D-ala D-lactate
Vancomycin typically only treats these types of infections (think broad here)
Gram positive organisms
Does vancomycin have good oral bioavailability?
No! Usually only given orally for C. diff infections because it stays in the GI tract (poorly absorbed from there)
Biggest side effect of vancomycin and how you treat it
“red man” syndrome due to histamine; treat by slow infusion and giving an antihistamine
This antibiotic is only given topically due to its severe nephrotoxicity. It inhibits phosphorylation/dephosphorylation cycling of lipid carriers that transfer peptidoglycan to cell wall
Bacitracin
What compound do sulfonamides antagonize?
PABA (para-amino benzoic acid)
MOA of sulfonamides
Structural analogs of PABA which inhibit dihydropteroate synthase. Stops the 1st step in synthesis of tetrahydrofolic acid
Adverse effects of sulfonamides
N/V, phototoxixity, HEMOLYSIS IN G6PD DEFICIENT
Why are sulfonamides contraindicated in neonates?
They displace bilirubin from albumin causing kernicterus.
Prototype of the sulfonamide drugs
sulfamethoxazole
Antibiotics that work synergystically with sulfonamides by preventing the next step in folate synthesis
Trimethoprim or pyrimethamine
MOA trimethoprim
Competitive inhibitor of dihydrofolic acid reductase
adverse effects of trimethoprim
Leukopenia, granulocytopenia, thrombocytopenia, megaloblastic anemia
The trimethoprim/sulfamethoxazole combo (TMP/SMX) is used mostly for these 2 types of infections
UTI and URI
used as prophylaxis/tx in Pneumocystis jirrovechi
What is premarin used for?
vasomotor symptoms assoc with menopause; vulvar and vaginal atrophy and abnormal uterine bleeding
What are the therapeutic uses of estrogen?
Contraception, hormone replacement therapy, female hypogonadism, dysmenorrhea, acne, osteoporosis
How do estrogens affect serum lipids?
Increased triglycerides and HDL
Decrease LDL
How is estrogen useful in preventing osteoporosis?
Decreases bone resorption
What are the adverse effects of estrogen?
N/V, headache, breast tenderness, endometrial hyperplasia, cholestasis, increased coagulation, endometrial cancer risk, increased breast cancer risk
Estrogen is contraindicated in which settings?
History of DVT, PE, recent MI or stroke, Breast cancer, pregnancy, hepatic dysfunction
Why does estrogen work as a contraceptive?
Suppresses ovulation
Fertility drug that is an antiestrogen; it induces ovulation by shutting down negative feedback to hypothalamus thus increasing FSH and LH. Biggest side effect is multiple births and hot flashes
Clomiphene
Therapeutic uses of progestins
contraception, HRT w/ estrogens, control of uterine bleeding, dysmenorrhea, suppression of postpartum lactation, endometriosis
Adverse effects of progestins
edema, depression, glucose intolerance, acne, hirsutism, breakthrough bleeding, decreased HDL and increased LDL
Progesterone antagonist used for abortion, adverse effects are cramping, bleeding, infection, ectopic pregnancy
Mifepristone RU486
How do progestins work as contraceptives?
prevents implantation to endometrium, increases thickness of cervical mucus
Two SERMS (selective estrogen receptor modulator)
Raloxifene and Tamoxifen
What is raloxifene used for?
prevent and tx postmenopausal osteoporosis by acting as an estrogen agonist in bone (antagonist in breast and uterus)
What is tamoxifen used for?
Breast cancer; acts as an estrogen antagonist in the breast (partial agonist in uterus thus increasing endometrial cancer risk)
suffix of floroquinolone antibiotics
-floxacin
Why are floroquinolone abx contraindicated in kids?
They hinder cartilage development, causing tendon rupture
4 main classes of beta lactam antibiotics
Penicillins, Cephalosporins, Carbapenems, Monobactams
Most common mechanism for beta lactam resistance
Beta lactamases which cleave the B lactam ring
Which class of Beta lactams is resistant to Beta Lactamases?
Monobactams
Most common example of a monobactam
Aztreonam
In the treatment of enterococcal and pseudomonal infections, penicillins are synergistic with what other class?
Aminoglycosides (penicillins alter the cell wall so they can enter)
3 Beta lactamase inhibitors that can be used with penicillins
Clavulanate, sulbactam, tazobactam
First generation cephalosporins (5)
Cefazolin, cephalexin, cefadroxil, cephapirin, cephadrine
Second generation of cephalosporins are different from 1st in what way?
Increased gram negative coverage
Second generation cephalosporins (5)
Cefuroxime, cefotetan, cefaclor, cefoxitin, cefprozil
How are 3rd generation cephalosporins different than 2nd?
Continued gram negative coverage and better able to cross BBB
Third generation cephalosporins (3)
Cefotaxime, Ceftazidime, Ceftriaxone
How are 4th generation cephalosporins different than 3rd/
increased beta lactamase resistance
Only representative drug of 4th generation cephalosporins
Cefepime
What is the mechanism of action of aminoglycosides?
Bind to 30s ribosomal subunit to prevent formation of the initiation complex, incorporating incorrect amino acids in the peptide chain
Examples of aminoglycosides (5)
Gentamycin, tobramycin, streptomycin, amikacin, neomycin
Side effects of aminoglycosides
Nephrotoxicity (ATN) and ototoxicity
Mechanism of action of clindamycin
Binds 50s ribosomal subunit to inhibit translocation of t-RNA from acceptor site to donor site
Major adverse effect of clindamycin
C. diff
MOA of macrolides
Binds to 50s subunit to inhibit translocation of t-RNA (like clindamycin)
Examples of macrolide antibiotics (3)
Erythromycin, Azithromycin, Clarithromycin
Why is 1 dose of Azithromycin just as effective of a 7 day course of doxycycline for treating chlamydia?
Azithro has a very long half life (68 hrs)
MOA of tetracyclines
Binds to 30s subunit to inhibit attachment of aminoacyl t-RNA to its acceptor site
What is the tetracycline demeclocycline used for?
SIADH because it inhibits ADH receptors in the collecting ducts
Some adverse effects of tetracyclines
Phototoxicity, hepatotoxicity, vestibular toxicity
Why are tetracyclines contraindicated in kids?
Tooth enamel dysplasia, permanent tooth discoloration, decreased bone growth via chelation with calcium salts
Oral absorption of tetracyclines can be impaired by what 4 minerals?
Iron, calcium, magnesium, aluminum
MOA of chloramphenicol
binds 50s subunit and inhibits peptidyl transferase
Adverse effects of chloramphenicol
Grey baby syndrome (ashen appearance, hypotension, vomiting, flaccidity)
Aplastic anemia
MOA of linezolid and what does it treat?
Binds 50s subunit and prevents formation of the initiation complex
treats MRSA and VRSA
MOA of rifampin
Inhibits DNA dependent RNA polymerase
MOA of isoniazid
inhibits mycolic acid synthesis
Adverse effects of rifampin
Red discoloration of tears, sweat and urine
hepatitis, elevated LFT’s
thrombocytopenia
Adverse effects of Isoniazid
Drug induced SLE Peripheral neuropathy (give B6!) hemolytic anemia in G6PD deficiency
Adverse effect of pyrizinamide
Phototoxicity, hepatitis, arthralgias
Adverse effects of ethambutol
red-green color bliindness, optic neuritis, decreased visual acuity
2 Polyene antifungals that bind to ergosterol and disrupt membrane permeability.
Amphotercin B and nystatin. (amphotercin B must be given intrathecally for CNS infections)
Mechanism of action of the -azole antifungals
Prevent synthesis of ergosterol by inhibiting cyp 450 dependent demethylation
Adverse effect of ketoconazole also associated with spironolactone
gynecomastia
The absorbtion of ketoconazole is increased by what and decreased by what?
Increased by phosphoric acid (colas) and decreased by antacids.
What will happen to the INR of a patient on warfarin who goes on an -azole?
Increased INR because azoles inhibit p450, decreasing the metabolism of warfarin and increasing blood levels.
antifungal only active against dermatophytes that deposits in newly formed keratin and disrupts the microtubule structure
griseofulvin: AE= hepatotoxicity
viral enzyme that adds phosphate to acyclovir to make it active
viral thymidine kinase
MOA of acyclovir
competes for viral polymerase, incorporated into viral DNA and terminates the chain
DOC for acyclovir-resistant HSV and VZV and ganciclovir-resistant CMV
Foscarnet (pyrophosphate analogue that inhibits viral RNA and DNA polymerase)
Amantidine is the DOC for what virus?
Influenza A only
Amantidine is used in what non-infectious disease process?
Parkinson Disease, drug induced extra-pyramidal symptoms, increases dopammine levels
Neuraminidase inhibitors that treat Influenza A and B
Zanamivir and Oseltamivir
Ribavirin is the DOC in what virus and what is its black box warning?
Treats RSV in infants but it is Pregnancy category X and extremely teratogenic
List the NRTI’s, and their main adverse effect
Zidovudine (AZT), Stavudine, Lamivudine, Didanosine, Abacivir and Emtricitabine. Main adverse effect is lactic acidosis.
If hypersensitivity is suspected, which NRTI should you immediately stop and never use again?
Abacavir
Antiretroviral agent that can cause Fanconi syndrome?
Tenofovir
NNRTI that causes abnormal dreams, impaired concentration and dizziness
Efavirenz
MOA is inhibiting fusion of HIV 1 and CD4 by blocking gp41 required for entry
Enfurvitide
Examples of protease inhibitors and major adverse effects
Atazanavir, lopinavir, ritonivir. Adverse effects are hepatotoxicity and fat redistribution
MOA of metronidazole and adverse effects
inhibit protein synthesis and cause DNA strand breakage. Adverse effects are N/V, disulfram reaction
Drug of choice for relapsing forms of Plasmodium vivax and ovale
Primaquine (causes hemolytic anemia in G6PD def patients)
Adverse effect of quinidine
Cinchonism
DOC for trematode (fluke) infections
Praziquantel
DOC for nematode (roundworm) infections
Mebendazole/Albendazole or Pyrantel Pamoate
DOC for African river blindness (Onchocerca volvulus)
Ivermectin
Toxicity of Doxorubicin and how you prevent it
Dilated Cardiomyopathy, prevent with Dexrazoxane
Toxicity of Bleomycin
pulmonary fibrosis
Toxicity of Cyclophosphamide and how you prevent it
Hemorrhagic cystitis and prevent with Mesna
Toxicity of Cisplatin
Nephrotoxic and prevent with Amifostene
Toxicity of vincristine
peripheral neuropathy
Drug used to prevent megaloblastic anemia in patients taking Methotrexate
Leucovorin, replenished folic acid in normal cells
6 MP levels are increased in patients also taking this drug
Allopurinol. 6 MP is metabolized by xanthine oxidase.
MOA of Vincristine/Vinblastine
Vinca alkaloids that inhibit polymerization of tubulin so microtubules cannot form
MOA of Paclitaxel
Binds to tubulin and stabilizes the microtubule, preventing depolymerization.
Neuronal release of Acetylcholilne into the synapse is inhibited by what toxin?
Botulism
Muscarinic receptor located on heart
M2 (Gi coupled, inhibits cAMP)
Muscarinic receptor located on smooth muscle, glands, GI tract, eye, bladder.
M3 (Gq coupled, IP3/DAG)
Effect of Ach on the eye
Contracts the ciliary muscle to increase accomodation, contracts the circular muscle of the iris to constrict the pupil.
Examples of muscarinic agonists
Bethanechol (urinary retention), carbachol, pilocarpine (both for lowering IOP in glaucoma)
Reversible Acetylcholinesterase inhibitors
Neostigmine, pyridostigmine, physostigmine, edrophonium, rivastigmine, donezipil, galantamine (these last 3 cross the BBB and are used to increase acetylcholine levels in the brain in Alzeheimer’s)
Short acting AChE inhibitor used to diagnose Myasthenia Gravis
Edrophonium (tensilon)
What do you give for an Atropine overdose?
Physostigmine
Examples of IRREVERSIBLE Acetylcholinesterase inhibitors
Echothiophate, sarin, malathion, parathion (Organophosphates)
Drugs used to treat Organophosphate poisoning
Atropine and Pralidoxime. Atropine binds the muscarinic receptors and outcompetes the ACh. Pralidoxime reactivates inhibited AChE.
What plant does Atropine come from?
Belladonna, “deadly nightshade”. Previously used to make girls look pretty by dilating their eyes and flushing their cheeks.
Therapeutic indication of Scopalamine
Motion sickness
Anticholinergic agents used to treat asthma and COPD
Ipratropium and tiotropium
Most commonly used Neuromuscular blocking drug
Succinylcholine. Used for endotracheal intubation because its fast onset and short duration.
Adverse effect of succinylcholine
Malignant hyperthermia (rigidity, increased CO2, tachycardia and hyperthermia)
Tx malignant hyperthermia
Dantrolene - inhibits calcium release from the SR of muscle cells, relaxing tone and reducing heat production.
MOA of reserpine
inhibits the transport of Norepi from the cytoplasm into the synaptic vesicles.
How does cocaine increase Norepi levels in the synaptic cleft?
inhibits the reuptake of Norepi back into the presynaptic neuron.
examples of alpha 2 agonists
Clonidine and alpha methyldopa
What is dobutamine used for?
Increases cardiac output in CHF without affecting the renal blood flow.
Drugs used for alpha blockade before and during removal of a pheochromocytoma
Phentolamine and phenoxybenzamine
selective alpha 1a antagonist used to treat BPH that has less cardio side effects than traditional alpha 1 antagonist
Tamulosin (less reflex tachycardia)
mixed alpha1/beta antagonists
Carvedilol and labetalol
Beta blockers with Intrinsic sympathomimetic activity
Acebutolol and pindolol
why are beta blockers used with caution in diabetics?
they can mask the symptoms of hypoglycemia
IFN alpha is used to treat what?
Chronic Hepatitis C (with ribavirin), Chronic Hep B, melanoma
IFN beta is used to treat what?
MS
DOC for H. pylori ulcer
PPI and 2 antibiotics (Clairthromycin and amoxicillin) If initial therapy fails, give PPI, bismuth sulfate, tetracycline and metronidazole.
DOC for acute variceal bleeding
Octreotide (somatostatin) decreases portal pressure and splanchnic flow. Next step in therapy is band ligation if this doesn’t work. Also used to treat acromegaly, carcinoid syndrome and glucagonoma.
DOC for hepatic encephalopathy
lactulose: lowers pH of the bowel and changes ammonia to ammonium which is excreted.
drug used to prevent recurrent variceal bleeding
propranolol
DOC for diabetic gastroparesis
Erythromycin or metoclopramide
Initial therapy for Crohn disease
mesalamine derivatives which best deliver 5-ASA to the affected area. (Asacol, Pentasa, Sulfasalazine). If it is not controlled, add the oral steroid budesonide or azahioprine.
1st line tx for Barrett esophagus
PPI
elevated liver enzymes, antimitochondrial antibodies point to Primary Biliary Cirrhosis which is best treated with what?
Ursodeoxycholic acid
Halothane, Nitrous oxide and Isoflurane are examples of what type of anesthetic?
Inhaled
What do inhaled anesthetics do to the cerebral vascular flow?
increase the flow
Which inhaled anesthetic is most closely associated with malignant hyperthermia?
Halothane (it also slows the heart rate)
Propofol, Ketamine, Fentanyl, Midazolam, Thipoental and Etomidate are examples of what type of anesthetic?
IV
Type of amnesia caused by midazolam
Anterograde amnesia
If you are allergic to these 2 foods, you cant have Propofol
Eggs and Soy
What type of amnesia is caused by Ketamine?
Dissociative amnesia (also vivid dreams and hallucinations)
IV anesthetic with antiemetic properties
Propofol
Examples of Amide local anesthetics
Lidocaine, Buprivicane, prilocaine, Mepivacaine (Amide locals all have 2 i’s)
Examples of Ester local anesthetics
Cocaine, Benzocaine, Procaine (Ester locals have 1 i)
What do opioids do to the pupils?
Constrict them - except Meperidine. (common sign of overdose)
Opioid analgesic used to prevent withdrawal symptoms in patients discontinuing heroin
Methadone. Also clonidine, a central alpha 2 agonist can help.
What do Benzodiazepines do to the chloride ion channels?
Increase the frequency they are open
What do Barbituates do to the chloride ion channels?
Increase the duration they are open
Which Benzodiazepine is also known as the “date rape drug?”
Flunitrazepam (rohypnol)
Longest acting Benzodiazepine
Diazepam (valium)
Adverse effects of benzodiazepines
Cnfusion, sedation, ataxia, cognitive impairment, amnesia, respiratory depression
What is phenobarbital commonly used to treat?
Generalized tonic clonic and partial seizures
Barbituates cause a lot of drug-drug interactions because they do this to P-450
Induce it
Adverse effects of barbituates
Sedation, impaired cognition, nausea, dizziness, increased heme synthesis, coma, respiratory depression, cardiovascular depression, addiction
Drug class used to prevent barbituate withdrawal
long acting benzos
Partial agonist at 5-HT 1A receptors, effective in treating generalized anxiety disorder
Buspirone
Mechanism of action of MAO inhibitors and 3 examples
Inactivate MAO therefore increasing levels of Serotonin, dopamine and Norepi in presynaptic neurons. Examples are Phenelzine, Isocarboxazid, and Tranylcypromide (treat atypical depression)
What life threatening event can happen if you take an MAOI with an SSRI?
Serotonin syndrome (rigidity, diaphoreis, hyperthermia, seizures, myoclonus)
MOA of Tricyclic (amitryptyline, doxepin, clomipramine and imipramine
Inhibits reuptake of 5HT and NE into presynaptic neurons and increase their levels in the synaptic cleft
TCA used to prevent nocturnal enuresis
imipramine
Adverse effect of TCA’s and how you treat its toxicity
Xerostomia, blurry vision, urinary retention, cardiac arrhythmias, seizures, sedation. Treatment of toxicity is Sodium Bicarb, activated charcoal to absorb from the GI and phenytoin for the seizures
What is the biggest adverse effect with Trazodone?
Priaprism
MOA of Buproprion
inhibits DA, 5HT and NE reuptake. Used in smoking cessation and OCD.
What class of drugs is Duloxetine (cymbalta) and Venlafaxine (effexor)?
SNRI (inhibits reuptake of only serotonin and norepi)
Which class of drugs is Fluoxetine (prozac), Paroxetine (paxil), Sertraline (zoloft), Citalopram (celexa), Escitalopram (lexapro)?
SSRI
(sorry for the trade names if you’re studying this but it helps me remember the classes)
(only affects serotonin reuptake)
Fluoxetine is used in these other clinical settings? (3)
Bulimia, panic disorder, PMDD
Adverse effects of SSRI’s (3)
Sexual dysfunction, agitation, anxiety
SSRI FDA approved for PTSD, social anxiety disorder
Paroxetine
DOC for treating Bipolar disorder (manic-depression)
Lithium
Adverse effects of lithium (7)
Acne, seizures, ataxia, visual disturbances, Drug induced nephrogenic diabetes insipidus, hypothyroidism, tremor
Drug to treat lithium induced nephrogenic DI
Amiloride (normally you give Thiazide diuretics for nephrogenic DI but not for lithium induced)
What enzyme does lithium inhibit to cause hypothyroidism?
5-deiodinase
Congenital heart defect associated to babies born to mothers taking lithium
Ebstein anomaly (malformation of tricuspid valve)
Other medications (mood stabilizers) that can be used to treat bipolar disorder (5)
Carbamazepine, valproic acid, benzos, gabapentin, topiramate
MOA of “typical” antipsychotics
inhibition of D2 receptors in mesolimbic system
MOA of “atypical” antipsychotics
Inhibition of 5-HT2 receptors
Examples of typical antipsychotics (4)
Haloperidol, chloropromazine, thioridazine, fluphenazine
Examples of atypical antipsychotics (4)
Clozapine, risperidone, olanzapine, quietapine
Medications used to treat antipsychotic-induced EPS (2)
Benztropine, amantidine
How do antipsychotics cause prolactinemia?
Inhibit Dopamine receptors in the anterior pituitary leading to unapposed prolactin
What is a potential life threatening adverse effect of antipsychotics?
Neuroleptic malignant syndrome. (Hyperthermia, rigidity, altered mental status, cardiovascular instability)
Treatment for Neuroleptic malignant syndrome
Dantrolene and Bromocriptine
2 antimuscarinic drugs used in the treatment of Parkinson’s (decrease acetylcholine)
Benztropine and Trihexyphenidyl
MAOb inhibitor used as a first line treatment in PD
Selegline (inhibits Dopamine metabolism in presynaptic neurons)
MOA of tolcapone and entacapone
Inhibit peripheral COMT thereby increasing the CNS uptake of L-dopa
MOA of carbidopa
Inhibits peripheral dopa-decarboxylase thereby increasing the amount of L-dopa available to CNS, allowing for lower doses of Levodopa needed.
What dietary restrictions should a patient on levodopa have?
Low intake of leucine and isoleucine (compete in GI for absorption) and no Vit B6 (pyridoxine) supplements because it enhances peripheral metabolism of levodopa.
MOA of phenytoin
Inhibit axonal sodium channels in the inactivated state to produce membrane stabilization
Adverse effects of phenytoin
Diplopia, ataxia, gingival hyperplasia, Steven Johnson, Nystagmus and teratogenic causing cleft lip and palate
Congenital defects caused by carbamazepine
Neural tube defects and craniofacial abnormalities
MOA of valproic acid
Inhibits axonal sodium channels and T type Calcium channels
Adverse effects of Valproic acid
Hepatotoxic, pancreatitis, photosensitivity, tinnitus, alopecia neural tube defects
Antiepileptic safe to treat partial and tonic-clonic seizures in pregnancy
Phenobarbital
Newer antiepileptic also used in migraines and neuropathic pain that inhibits carbonic anhydrase
topiramate (inhibits glutamate AMPA receptors and increases GABA effects)
MOA of Sumatriptan
5-HT 1D agonist which causes vasoconstriction in cranial arteries (don’t use in angina patients)
Class 1a antiarrhythmics (3)
quinidine, procainamide, disopyramide
class 1b antiarrhythmics (3)
Lidocaine, mexiletine, phenytoin
Class 1c antiarrhythmics (2)
Flecainide, propafenone
Class II antiarrhythmics (class)
Beta blockers (propranolol, esmolol)
Class III antiarhythmics (3)
Amiodarone, sotalol, dofelitide
Class IV antiarrhythmics (2)
Verapamil and diltiazem
3 antiarrhythmic drugs that do not fit into this classification
Adenosine (SVT, PSVT), digoxin (A-fib and flutter), magnesium (TdP)
Drugs that can cause Drug induced Lupus
Procainamide, Hydralazine, Isoniazid, sulfasalazine, methyldopa
What type of arrhythmia is lidocaine useful in?
Ventricular. Does not treat atrial.
Pulmonary fibrosis, arrhythmias, Hypo/hyperthyroidism, SIADH, optic neuritis, hepatotoxicity, blue skiin discoloration are all side effects of what antiarrhythmic?
Amiodarone
What type of arrhythmia should verapamil never be given in?
WPW syndrome because it causes an AV block leading to unopposed accessory pathway
What effects does digoxin have on contractility, heart rate and AV conduction velocity?
Increases contractility, Decreases rate and conduction velocity
adverse effects of digoxin
arrhythmias, blurred vision, haloes around light sources, n/v/ha
Drugs that can increase digoxin concentration
Quinidine, amiodarone, erythromycin, verapamil
Drugs that can decrease digoxin concentrations
diuretics, steroids
2 Beta blockers with specific indications for CHF
Metoprolol and Carvedilol (mixed alpha/beta blocker)
What will thiazide diuretics do to the serum calcium?
Increase it.
What do loop diuretics do to serum calcium?
Decrease it
Adverse effects of Thiazides (7)
Hypercalcemia, hyperuricemia, hypokalemia, alkalosis, hyperlipidemia, hypomagnesmia, hyperglycemia
Adverse effects of loop diuretics (6)
Hypocalcemia, hypokalemia, hypomagnesimia, alkalosis, hyperuricemia, ototoxicity
MOA of carbonic anhydrase inhibitors
increases excretion of sodium and bicarbonate (used to treat altitude sickness and glaucoma)
Adverse effects of beta blockers (6)
Hypotension, lipid abnormalities, rebound HTN upon withdrawal, sexual dysfunction, fatigue, hyperglycemia, depression
Adverse effects of ACE inhibitors
Hypotension, dry cough, angioedema, hyperkalemia
ACE inhibitors are contraindicated in what 2 settings?
Pregancy and bilateral renal artery stenosis
Adverse effects in CCB’s (block L type Ca channels)
Headache, constipation, (reflex tachy and peripheral edema in DHP’s and AV block in NDHP’s)
Adverse effects of statins
Increased LFT’s, rhabdomyolysis, myalgia, contraindicated in pregnancy
Drug used to increase HDL
Niacin (b3-nicotinic acid)
Drug used to mainly decrease Triglycerides
fibrates (activate lipoprotein lipase) can cause cholelithiasis
Drugs that inhibit platelet aggregation by blocking ADP receptors (2)
Clopidogrel and Ticlopidine
MOA of heparin
Binds to antithrombin III to inactivate intrinsic system of clotting cascade. Measure heparin by the PTT
Drug that selectively inhibits factor Xa
Fondaparinaux
MOA of Warfarin
inhibits synthesis of vitamin K dependent clotting factors II, VII, IX and X, protein C and S (extrinsic system, measure by PT/INR)
MOA of abciximab, tirofiban and epifibatide
Blocks glycoprotein IIb/IIIa thus inhibiting platelet aggregation
Drug that can counteract TPA
Aminocaproic acid
How do corticosteroids treat asthma?
decrease production and release of cytokines, decrease vascular permeability, decrease mucus production, decrease inflammatory cell activation, recruitment and infiltration
How do mast cell stabilizers treat asthma? (cromolyn)
prevent mast degranulation, decreasing release of histamines and leukotrienes
How do 5-lipoxygenase inhibitors treat asthma? (Zileuton)
inhibits leukotriene production from arachodonic acid, preventing bronchoconstriction
1st line for COPD treatment
Inhaled anticholinergics (ipratropium)
DOC for cough suppression
Dextramethorphan (no analgesia or addiction)
medications that can be used to accelerate fetal lung maturity
Glucocorticoids, TRH
How does N-acetylcysteine reduce accumulation of viscous mucus in CF patients?
breaks disulfide bonds in mucoproteins thereby lowering viscosity
MOA of metoclopramide
D2 antagonist that increases LES pressure and accelerates gastric emptying in GERD treatment
Also blocks centrally in the CTZ to act as an antiemetic
Adverse effects of PPI’s
bacterial overgrowth in GI, association with hip fractures
3 mediators that can stimulate gastric acid secretion from parietal cells
Gastrin, Acetylcholine, Histamine
Treatment of NSAID induced peptic ulcers
Prostaglandins (because they also stimulate secretion of bicarb and mucus to protect the lining) (misoprostol)
Sulfasalazine (aminosalicyclate) is cleaved by colonic bacteria into what 2 compounds?
Sulfapyridine (antibiotic) and Mesalamine (5-ASA)
5-ASA is first liine in treating what?
IBD
MOA of infliximab (which treats IBD)
binds to TNF alpha
MOA of Odansetron, dolasetron, granisetron
5-HT3 receptor antagonists
Other than blood glucose regulation, insulin can be used to treat what?
Hyperkalemia because it causes K to move into cells.
MOA and side effects of sulfonylureas (tolbutamide, glyburide, glimerpiride)
Block ATP dependent K channels which depolarizes beta cells causing a calcium mediated insulin release. Adverse effects are hypoglycemia and weight gain.
MOA and side effects of Thiazolidinedones (rosiglitazone, pioglitazone)
Bind to PPAR gamma which increases sensitivity to insulin and upregulates insulin receptors. Side effects are edema, CHF, weight gain, hepatotoxicity, bone fractures.
MOA and side effects of biguanides (metformin)
Decrease hepatic gluconeogenesis and increase sensitivity to insulin. Adverse effects are diarrhea, lactic acidosis and decreased B12
MOA and side effects of alpha glucosidase inhibitors (Acarbose and miglitol)
Inhibit intestinal amylase and alpha glucosidase, delaying carbohydrate breakdown and glucose absorbtion. (only good for postprandial) Side effects are flatulence, bloating and cramping
Drug with positive inotrope and chronotrope activity used to stimulate the heart during Beta Blocker overdose
Glucagon
What are some drugs that can cause Nephrogenic Diabetes insipidus?
Lithium, demeclocycline, vincristine, amphotercin B
DOC for central DI
Desmopressin (DDVAP)
SE of desmopressin
Water intoxication, hyponatermia, headache
DOC for SIADH
demeclocycline
DOC for hyperthyroidism
PTU and methimazole; PTU in pregnancy
Drug used to diagnose adrenal insufficiency
ACTH (cosyntropin)
Which drug inhibits glucocorticoid synthesis by inhibiting 11 hydroxylase?
Metyrapone
Antifungal that can also be used to lower cortisol levels in cushings disease and could cause gynecomastia
Ketoconazole
Androgen receptor blocker that is used in the treatment of prostate cancer
Flutamide
MOA of clomiphene
induces ovulation by inhibiting negative feedback of estrogen on the hypothalamus and pituitary leading to more LH and FSH release
MOA of tamoxifen
Estrogen agonist in bone and uterus, estrogen antagonist in breast (used for breast cancer)
Difference between tamoxifen and raloxifene
Raloxifene is an antagonist in the uterus and does not cause endometrial hyperplasia and increase endometrial cancer risk
PGE1 analog used for impotence
Alprostadil
PGF2a analogs promoting bronchiolar and uterine smooth muscle contraction
Carboprost and dinoprost
PGI2 analog (prostacyclin) that is used for pulmonary HTN
Epoprostenol
MOA of acetamminophen
inhibits prostaglandins via COX 3 in CNS
Metabolite of acetaminophen that is hepatotoxic
NAPQI; gluthianone is responsible for its removal
3 medications known to cause gingival hyperplasia
Cyclosporine, Phenytoin, Nifedipine
MOA of cyclosporine
complexes with cyclophilin to inhibit calcineurin which decreases IL-2 thereby T cell activation
MOA of tacrolimus
Inhibits calcineurin by binding to FK binding protein, also inhibiting IL-2
Immunosuppressant that acts by inhibiting inosine monophosphate dehydrogenase thereby inhibiting de novo guanine synthesis
Mycophenolate mofetil
Why was the weight loss drug fen-phen taken off the market?
Pulmonary HTN
suffix of bisphosphonate drugs
-dronate
MOA of bisphosphonates
Inhibition of osteoclast mediated resorption of bone
MOst common side effect of allopurinol
Skin rash
Treatment of acute gout
Colchicine and an NSAID
MOA of isotretinoin (accutane)
decreases sebaceous gland size and decreases sebum production
antidote for arsenic, gold, alopecia, lead and mercury
dimercaprol
antidote for iron poisoning
deferoxamine
Signs and symptoms of arsenic poisoning
Rice water stools, seizures, pallor, skin pigmentation, stocking glove neuropathy
Signs and symptoms of mercury poisoning
ataxia, hearing loss, visual loss, chest pain, renal failure, n/v
Signs and symptoms of TCA poisoning
Hyperthermia, coma, convulsions, cardiotoxicity, dilation of pupils, constipation, prolonged QT