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205 Cards in this Set

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What do you develop w/ benzodiazepines use? What receptors?


down-regulation of B2 receptors
Initial Tx for Status Epilepticus?
1) Diazepam
2) Lorazepam
What drug causes sedation, ataxia and diplopia?

What is SAD Sx and who produces it?
sedation, ataxia and diplopia

What drugs causes gingival hyperplasia?
1) Phenytoin
2) Nifedipine
3) Cyclosporin
CNS drugs

CNS drugs...

Name the anticonvulsant that is degraded in zero-order?
What drug is used for tx of abscence seizure?
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...
Name the drug that causes megaloblastic anemia and decreases folic acid?
What anticovulsant causes SIADH?
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?
DOC for trigeminal neuralgia?
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
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?
Tx for Status Epilepticus (I.V.)?
What drug is used for relaxation and detoxification for withdrawal states?
Antidote for Zolpidem overdose?
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?
What drug acts in the BZ1 receptor but it's not a benzodiazepine?
What is the action of barbiturates [high dose]?
increase duration Cl-

opens Cl- channels
blocks Na+ channels

increases duration of Cl- open
What is the mechanism of Buspirone?
- no gaba
- partial agonist at 5HT1a

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?
What is methanol degraded to?

- alcohol dehydrogenase
What is the lethal dose of methanol?
5 ounces
What is the toxic retinal dose of methanol?
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
What are felbamate, lamotrigine and gabapentin used for?
Neuropathic pain
Name the 3 new Anticovulsants?
Name 3 drugs used in complex seizure tx?
Valproic Acid
Tx for Generalized Anxiety States (GAS)?
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)

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?
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?
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
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

A first letter of the alphabet
What drug has the mechanism of inhibiting peptidyl transferase?
What drug inhibits aminoacyl-tRNA binding to A site?

t is for tRNA
What drug inhibits the translocation of tRNA?
What bacteria have the same mechanism of action as macrolides?
diphtheria toxin
pseduomonas toxin
What drug is an Angiotensin II blocker?
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?

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
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)
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?
Where is does the reaction L-Arg to NO take place?
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?
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?
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?
What part of the nephron do thiazides act in?
Distal Convoluted Tube

What is used in HTN and Heart Failure (CHF)?
What happens to ions in blood after thiazide administration?
What are thiazides used for?
What are the toxicities of hydrochorothiazides?

sulfa allergies
What does hyperGLUC stand for?
Sulfa Allergies
What is the potential toxicity of K+-Sparing Diuretics?
endocrine effects like GYNECOMASTIA!
Diuretic that causes hyperglycemia?
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?
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
What is the only lipid friendly thiazide?
What diuretics are in the sulfa family?
What diuretic works on ATII? Aldosterone receptor blocker?
What mechanism does Spirinolactone use? (protein)
acts via Zinc Finger Protein

increases gene expression
increases Na+ Channels to open
What diuretic causes ginecomastia?
Diuretic that causes hypoCAlcemia?

Loops Loose Calcium

Tx malignancies with it!
Diuretic that causes hyperCalcemia?
Pharmacology Kaplan
What drug do Loop diuretics interfere with?
Lithium decreases clearance and increases lithium in serum
What drug potentiates OTOtoxicity w/ Loop diuretics?
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?
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?
What drug causes flushing, sedation, dyspnea and only acts for t1/2 30 sec?
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?
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
It's a cholinomimetic, AchE inhibitor, contracts ciliary m., increases outflow?
Pilocarpine and ECHOthiopate
What are Pilocarpine and Echothiopate used for?
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
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?
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?
What 2 drugs interact with digoxin (DDI)?
Quinidine and Verapamil (the queen and the rapper always interfere)
Drug that causes phototoxicity?
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?
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?
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?
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?

Name an anticonvulsant that is Zero-Order?
What condition has an EEG with 3/sec spike pattern?
Generalized Abscence Seizure
What is the Tx for Generalized Abscence Seizure?
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?

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

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