Pharmacology from Kaplan
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- What do you develop w/ benzodiazepines use? What receptors?
-
Tolerance
down-regulation of B2 receptors - Initial Tx for Status Epilepticus?
-
1) Diazepam
2) Lorazepam - What drug causes sedation, ataxia and diplopia?
-
Phenytoin
SAD Sx. - What is SAD Sx and who produces it?
-
sedation, ataxia and diplopia
Phenytoin - What drugs causes gingival hyperplasia?
-
1) Phenytoin
2) Nifedipine
3) Cyclosporin - CNS drugs
- CNS drugs...
- Name the anticonvulsant that is degraded in zero-order?
- Phenytoin
- What drug is used for tx of abscence seizure?
- Ethosuximide
- What is the mechanism of action of ethosuximide?
- blocks Ca+ in thalamic neurons
- What drug do you use for preop sedation i.v.? It causes amnesia...
- Midazolam
- Name the drug that causes megaloblastic anemia and decreases folic acid?
- Phenytoin
- What anticovulsant causes SIADH?
- Carbamazepine
- What effect does carbamazepine have on the liver?
- it induces cyt P450 (+)
- What is the formula for minimal alveolar anesthetic concentration?
-
MAC= 1/(potency[lipid solubility])
Lipid = potency = 1/MAC - What anticonvulsant causes drug induced Ricketts or ostemalacia?
- Phenytoin
- DOC for trigeminal neuralgia?
- Carbamazepine
- What are 3 Side/Effects (S/E)of Carbamazepine?
-
1) Cyt. P450 inducer (+)
2) Hematotoxicity
3) increase ADH (retains water) - What is the effect of carbamazepine and Oral Contraceptives?
-
inactivates sex steroids and O.C.
lowers estriol - What is carbamazepine the DOC for?
- Trigeminal Neuralgia
- What effect does carbamazepine have on P450?
- induces it
- Name two important Side/Effects (S/E) of Carbamazepine?
-
1) hematotoxicity
2) SIADH - Drug used for Anxiety/Panic?
- A/P AlPrazolam
- Patien w/ depression needs to be treated but has liver failure? Tx pt. w/ which benzos...
-
1) Oxazepam
2) Temazepam
3) Lorazepam
Out The Liver - What are the three OUT THE LIVER Benzodiazepines?
-
Oxazepam
Temazepam
Lorazepam - Tx for Status Epilepticus (I.V.)?
- Lorazepam
- What drug is used for relaxation and detoxification for withdrawal states?
- diazepam
- Antidote for Zolpidem overdose?
- Flumazenil
- Where do benzodiazepines work?
-
GABAa receptor
gama binding site
BZ1 hypnotic (sleep)
increases frecuency of Cl- channel - What site do benzodiazepines act in?
-
gama binding site
BZ 1 - What drug is antagonist at the BZ receptor?
- flumazenil
- What drug acts in the BZ1 receptor but it's not a benzodiazepine?
- Zolpidem
- What is the action of barbiturates [high dose]?
-
increase duration Cl-
opens Cl- channels
blocks Na+ channels
barbiDURATES
increases duration of Cl- open - What is the mechanism of Buspirone?
-
- no gaba
- partial agonist at 5HT1a
-nonsedating -
What is the action of disulfiram? Whic cell compartment does it work on?
Increase what? -
inhibits acetaldehyde dehydrogenase
- mitochondria
- increases NADH - What is Methanol used for? (Tx)
-
- Ehtanol intoxication
- fomepizole - What is the definite Tx for ethanol/fomepizole intoxication?
- Dialysis
-
What is methanol degraded to?
Enzyme? -
formaldehyde
- alcohol dehydrogenase - What is the lethal dose of methanol?
- 5 ounces
- What is the toxic retinal dose of methanol?
- 5cc
- What does the Disulfiram Reaction consists of?
-
1) Nausea
2) Vomiting
3) Vertigo
4) Hypotension/Shock - What causes a 3/sec spike pattern on EEG?
-
Abscence seizure
Petite Mal - What is indicated in neuropathic pain?
-
1) Felbamate
2) Lamotrigine
3) Gabapentin - What are the S/E of Felbamate?
-
Aplastic Anemia
Acute Liver Failure - What are the S/E of Lamotrigine?
-
Steven-Jonhson Sx
Rash - What are felbamate, lamotrigine and gabapentin used for?
- Neuropathic pain
- Name the 3 new Anticovulsants?
-
Felbamate
Lamotrigine
Gabapentin - Name 3 drugs used in complex seizure tx?
-
Valproic Acid
Phenytoin
Carbamazepine - Tx for Generalized Anxiety States (GAS)?
- Buspirone
- How long do you wait for buspirone to take effect?
- 1-2 weeks
- What is divalproex used for?
- Bipolar Disorder (backup)
- What is the mech. of action (M/A) for Divalproex?
-
Ca+ block
inhibits GABA transaminase
axonal Na+ block - What are the A/E of Valproic Acid?
-
1) hePAtotoxicity
2) PAncreatitis
3) aloPEcia
4) sPIna Bifida (Teratogenic)
PA PE PI
VALPA PE PI - What combination w/ anticonvulsants have additive CNS depression?
-
1) antihistamines
2) ethanol
3) sedative-hypnotics
4) opioids - What happens if you withdrawal anticonvulsants abruptly?
- Seizure might be precipitated
- What is the Tx for Tonic-clonic seizure?
-
- Valproic Acid
- Phenytoin
- Carbamazepine - This is unique to collagen?
- hydroxyproline
- What is the defect in Ehlers-Danlos? name the gene
-
mutation of collagen gene
- lysine hydroxylase gene - What are the symptoms of Ehlers-Danlos
- hyperextensible, hypermobile joints, dislocations
- What is the defect in Menkes Dz?
-
inhibition of lysyl oxidase
Copper (Cu+) deficiency - What are the symptoms in Menkes Dz?
-
depigmented steely hair
decrease urinary Cu+ - What disease has mutation in collagen I?
- Osteogenesis Imperfecta
- What are the symptoms for Osteogenesis Imperfecta?
-
Pathologic Fractures
blue sclera
collagen problems - Patient with coarse facial features, gingival hyperplasia and macroglosia? Dx?
- I-Cell Dz
- What enzyme is deficient in I-Cell Dz?
- phosphotransferase
- Where in the cell is the problem in I-Cell Dz?
-
Golgi apparatus
Manose-6 Residues - What are the symptoms of I-cell Dz?
-
coarse facial features
gingival hyperplasia
macroglosia - Patient with deficiency in Leu, Ile and Val amino acids?
- Maple Syrup Dz
- What type of amino acids are Leu, Ile and Val?
- Branched Amino Acids
- What drug inhibits activation? binds to t-RNA with ribosome?
-
blocks initiation
Aminoglycosdies
A first letter of the alphabet - What drug has the mechanism of inhibiting peptidyl transferase?
- Chloramphenicol
-
What drug inhibits aminoacyl-tRNA binding to A site?
Elongation -
Tetracycline
t is for tRNA -
What drug inhibits the translocation of tRNA?
E.F.3 - Macr(ol)ides
- What bacteria have the same mechanism of action as macrolides?
-
diphtheria toxin
pseduomonas toxin - What drug is an Angiotensin II blocker?
- SARTANS
- What are the effects of Sartans on aldosterone, bradykinin, AT-1
-
decrease aldosterone
decrease bradykinin
increase AT-1 - What is the DOC (drug of choice) for CHF (Cardiac Heart Failure)?
- ACE inhibitor
- What effect does ACE have on ATII, bradykinin, aldosterone, fluid, preload, afterload?
-
decrease ATII
increase bradykinin
decrease aldosterone
decrease fluid
increase vasodilation
decrease preload
decrease afterload - What it the drug used for HTN causes dry cough and angioedema?
- PRILS [Ace(-)]
- Why do ACE(-) cause cough?
- increases bradykinin and causes edema in the pharynx
- What drug causes disorientation, visual effects (halos), hallucinations, SVTs, AV block?
- Digitalis Toxicity
- What enzymes increase cAMP in cardiac cells?
-
(+) adenylyl cyclase
(-) phosphodiesterase III - What is the mechanism of action of sildenafil?
-
blocks PDE V
(-) phosphodiesterase V
increases cGMP - What drug interacts with sildenafil?
-
Nitrous Oxide
since NO also increases cGMP - What is the mechanism of phosphodiesterase III? What cells are involved?
-
inhibits conversion of cAMP to AMP
so increase in cAMP
Cardiac Cell - What two drugs inhibit PDE III?
-
theophylline
inamirone - What is the mechanism of action of inamirone?
-
blocks cAMP to AMP
incrases cAMP inside cardiac cell
increases force of contractilily - What enzymes are deficient in vitamin C def?
- (-) prolyl and lysyl hydroxylase
- What part of the cell are prolyl and lysyl hydroxylase?
- inside the R.E.R.
- What is the mechanism of action of dobutamine and dopamine?
-
B1 receptor
increase adenylyl cyclase (+)
ATP----> increases cAMP
cAMP---> Protein Kinase
Protein Kinase opens Ca2+ channels
increase in Ca2+ - What is the mechanism of action of digoxin?
-
inhibits Na+/K+ ATPase
decreases sodium/Ca+ exchange
Ca+ stays inside the cell
to increase contraction force
inhibited by K+ increase - What 5 drugs/states cause digitalis toxicity?
-
1) quinidine
2) NSAIDS
3) Amiodarone
4) Verapamil
5) hypokalemia - What is the mechanism of phosphodiesterase V?
-
increases cGMP
blocks breakdown of cGMP--> GMP - What drugs/compounds stimulate Gq to IP3?
-
Acetylcholine (Ach)
Bradykinin
5HT - What happens to Gq after it is converted to IP3?
- releases Calcium
- What is Calciums effect on Nitrous Oxide?
- it stimulates the conversion of L-arg to NO
- What amino acid does Nitrous Oxide derive from?
- L-Arginine
- Where is does the reaction L-Arg to NO take place?
- endothelium
- What does NO do inside the smooth muscle?
- stimulates guanylate cyclase
- What does guanulate cyclase stimulate?
-
Conversion of GTP to cGMP
so increase cGMP - What other amino acid is involved in making NO?
- cysteine
- What does NO stimulate?
-
guanylate cyclase
and conversion of GTP to cGMP
increases cGMP - Where in the nephron does acetazolamide act?
- proximal convoluted tube
- What are the effects of acetazolamide?
- decreases HCO3-
- What are the toxic effects of acetazolamide?
-
metabollic acidosis
neuropathy, sulfa allergy - What happens to the urine with acetazolamide?
-
increase Na+ excresion
increases HCO3- excresion - What diuretic works in the collecting ducts?
- Potassium Sparing (K+) diuretics
- What are the K+ sparing diuretics?
-
Spirinolactone
Amiloride
Triamterene - How is Spirinolactone different from Amiloride and triamterene?
-
Spirinolactone is an Aldosterone receptor inhibitor
the other two are Na+ Channel blockers - What drug blocks Na+/Cl- symport in the renal system?
- Thiazides
- What part of the nephron do thiazides act in?
-
Distal Convoluted Tube
DCT - What is used in HTN and Heart Failure (CHF)?
- Thiazides
- What happens to ions in blood after thiazide administration?
-
Hypokalemia
Alkalosis
HyperCAlcemia - What are thiazides used for?
- HTN and CHF
- What are the toxicities of hydrochorothiazides?
-
hyperGLUC
sulfa allergies - What does hyperGLUC stand for?
-
hyperGlycemia
hyperLipidemia
hyperUricemia
hyperCalcemia
Sulfa Allergies - What is the potential toxicity of K+-Sparing Diuretics?
-
Hyperkalemia
endocrine effects like GYNECOMASTIA!
Anti-Androgen - Diuretic that causes hyperglycemia?
- Thiazide
- What is the mechanism for thiazide acting as hyperglycemia?
-
blocks insulin release
opens K+ Channels
keeps insulin inside b-cells - What diurectic causes alkalosis and hypoCalcemia?
- Loop diuretics
- What diuretic causes alkalosis and hyperCalcemia?
- Thiazide
- What diuretic causes acidosis and hyperKalemia?
- K+ sparing
- What diuretic causes acidosis and hypoKalemia?
- Carbonic Anahydrase inhibitors
- All diuretics cause what?
-
hypokalemia to a degree
except K+ sparing - What is the mechanism of CA(-) Carbonic anahydrase inhibitors?
-
NaHCO3 diuresis
HCO3- decreases in blood so causes H+ to be unbalanced
Acidosis - What is the only lipid friendly thiazide?
- Indapamide
- What diuretics are in the sulfa family?
-
CA(-)
Loops - What diuretic works on ATII? Aldosterone receptor blocker?
- Spironolactone
- What mechanism does Spirinolactone use? (protein)
-
acts via Zinc Finger Protein
increases gene expression
increases Na+ Channels to open - What diuretic causes ginecomastia?
- Spirinolactone
- Diuretic that causes hypoCAlcemia?
-
Loops
Loops Loose Calcium
Tx malignancies with it! - Diuretic that causes hyperCalcemia?
- Thiazides!
- Question
- Answer
- Pharmacology Kaplan
- Pharm
- What drug do Loop diuretics interfere with?
- Lithium decreases clearance and increases lithium in serum
- What drug potentiates OTOtoxicity w/ Loop diuretics?
- Aminoglycosides
- What drug interacts w/ Gemfibrozil?
- HMG-coA reductase inhibitors (statin drugs)
- What is the result of the DDI (drug drug interaction) of Gemfibrozil and Statin drugs?
- Rhabdomyolisis increases
- What drug potentiates Gemfibrozil?
- Warfarin and Sulfonylurea
- What drugs inhibit HMG-coA reductase?
- Statin drugs
- What effect do statin drugs have on cytochrome p450?
- increases p450 activity p450(+) inducer
- What is the effect of stain drugs on HDL and TGs?
- HDL increase and decrease in TGs (triclyerides)
- What are the A/E (adverse/effects) of statin drugs?
- myalgia/myopathy, rhabdomyolysis; p450(+) renal failure; death
- What antilipid drug causes flushing and pruritus (hepatotoxicity)?
- Nicotinic Acid
- What is the mechanism of action of Cholestipol and Cholestyramine?
- they are bile acid sequestrants that prevent reabsorption of bile salts in the GI tract
- What is the effect of decrease in bile acid?
- increase synthesis of new bile salts; decrease liver cholesterol; increase LDL receptors; decrease plasma LDL
- What is contraindicated w/ bile acid sequestrants?
- concomitant use with hypertriglyceridemias because they increase VLDL and TGs
- What do bile acid sequestrants DDI with?
- DDI digoxin and warfarin; decrease their absorption
- Does HMG-coA reductase cause SLE Sx?
- yes
- What ist the mechanism of action of nicotinic acid?
- inhibits VLDL synthesis and apoprotein synthesis
- What is good about nicotinic acid?
- increase HDL
- How do you treat the flushing and pruritus w/ nicotinic acid?
- ASA (aspirin)
- What is another adverse effect of nicotinic acid?
- hepatotoxicity
- What drug causes flushing, sedation, dyspnea and only acts for t1/2 30 sec?
- adenosine
- Adenosine is antagonized by?
- theophilline and caffeine
- Pharmacologist refer to adenosine as?
- Reset Button Dead for 30 seconds and then heart starts again
- DOC for PSVTs?
- adenosine
- What are the effects of adenosine on SA and AV?
- decrease SA and AV; increases AV refractory period
- What drug is an M blocker and is used for asthma and COPD? It has no CNS entry
- Ipratropium
- It's a cholinomimetic, AchE inhibitor, contracts ciliary m., increases outflow?
- Pilocarpine and ECHOthiopate
- What are Pilocarpine and Echothiopate used for?
- Glaucoma
- What are the three K+ channel blockers?
- Amiodarone, Bretylium and Sotalol ABS system
- What do K+ channel blockers do?
- slow phase 3, increase APD
- What is the mechanism of action of Quinidine?
- blocks Na+ channels (decrease I Na); increase APD and ERP; M blocker; alpha block
- DOC for arrythmias following cardioversion? I.V. use
- Lidocaine
- What is amiodarone used for?
- Atrial and Ventricular Arrythmias
- What are the S/E of Amiodarone?
- hepatic necrosis; PULMONARY FIBROSIS; Corneal Deposits; BLUE Pigmentation (SMURF) Skin; Photoxocity; Thyroid Dysfunction
- What is the t1/2 life of Amiodarone?
- 40 days; Largest Vd
- What is Manitol used for?
- 1) maintain renal function; 2) close angle glaucoma; 3) decrease intracraneal pressure (tumor, hematoma)
- Newborn w/ strabysmus, decrease growth, midfacil hypoplasia; microcephaly; CNS Dysfunction; Thin Upperlip (Phyltrum)
- Fetal Alcohol Syndrome
- What is Benztropine and Trihexyphenidyl used for?
- Parkinson's; Drug-Induced Extrapyramidal Dysfunction
- Mechanism of action of Benztropine and Trixehyphenidyl?
- M Blocker
- Drug used in organophosphate poisoning?
- Pralidoxime
- What does Pralidoxime do w/ symptoms?
- corrects patients labored breathing and decreases muscle weakness
- What is pralidoxime used for?
- Organophosphate Poisoning
- What drug is used for Parkinson and Drug-Induced Extrapyramidal Dysfunction?
- Benztropine and Trihexyphnidyl
- How does alcohol produce gout?
- Alcohol decreases NADH and increases NAD; increases conversion of reversible reaction pyr ---> Lactate; Lactate increases and competes w/ uric acid excrecion causing gout
- What biochemical compound is increased in alcoholism?
- NAD+
- What 2 drugs interact with digoxin (DDI)?
- Quinidine and Verapamil (the queen and the rapper always interfere)
- Drug that causes phototoxicity?
- Amiodarone
- Name 3 drugs used in AchE inhibitor poisoning?
- Malathion, Parathion and Sarin (nerve gas)
- What is the MOA of Hydralazine?
-
increase NO
increase Guanylate Cyclase
increase cGMP
relaxes vascular musculature - What is the effect of Hydralazine on TPR?
-
decreases TPR
involves NO/EDRF pathway
decreases resistnace in coronary, renal and cerebral beds - What is hydralazine used for?
- Tx for moderate to severe HTN
- What is Hydralazine metabolized by?
- N-acetyltransferase
- What are A/E of hydralazine?
-
headache, flushing, sweating and fluid retention
part of HIP
so SLE-like symptoms - What is used in HT emergency?
- Nitroprusside
- What is the effect of nitroprusside on TPR?
- decrease TRP via dilation of arterioles and venules
- What happens when there is venule dilation after nitroprusside use?
- Orthostatic Hypotension
- What are by-products of nitroprusside?
- thiocyanate and cyanide ions
- What part of the mitochrondria is damaged with cyanide compounds?
-
Comple IV (looks like N)
cyt. a/a3 - What is ethylene glycol?
- Anti-freeze
- What happens to ethylene glycol once ingested?
-
it is degraded to gycoaldehyde
- Alcohol Dehydrogenase is the enzyme - What comes after degradation of glycoaldehyde?
-
glycolic acid and oxalic acid
latter is nephrotoxic - What causes drug induced SIADH?
-
1) Carbamazepine
2) Chlorpropamide - What are the symptoms in Phenytoin Intoxication?
-
SAD Sx
Sedation
Ataxia
Diplopia - Name an anticonvulsant that is Zero-Order?
- Phenytoin
- What condition has an EEG with 3/sec spike pattern?
- Generalized Abscence Seizure
- What is the Tx for Generalized Abscence Seizure?
- Ethosuximide
- Name 4 drugs that block voltage gated axonal Na+ influx of fast channels?
-
1) Carbamazepine
2) Phenytoin
high dose:
3) Barbiturates
4) Valproic Acid - What drug decreases Ca2+ influx through T channels in thalamic neurons?
-
Ethosuximide
Valproic Acid -
What is the action on alpha 2 receptors?
1) NE
2) trasmitter release
3) platelets
4) Pancreas -
1) decrease NE synthesis
2) decrease transmitter release at prejunctional nerve terminals
3) increase aggregation of platelets
4) decrease insulin secretion
catabolism - Effect of B1 receptors on renin?
- increase renin release
- What adrenoreceptor increases insulin secretion?
- beta 2 receptor stimulation
- What adrenoreceptor induces glycogenolysis?
- B2 stimulation
- What adrenoreceptor causes uterine relaxation?
- B2 stimulation