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91 Cards in this Set

  • Front
  • Back
What is angina?
Chest pain on exertion. Can't supply the heart's demand for oxygen
What is CHF?
Heart doesn't pump hard enough due to damage from previous MI, and get edema (fluid in lungs..throughout body).
Define Myocardial Infarction

What two problems can it lead to later?
Heart attack. Deficiency in oxygen supply to heart, but some sections are getting NO OXYGEN. Get permanent tissue damage.

CHF and Cardiac Arrhythmias (especially ventricular)
What is the recommended ratio of LDL/HDL?
Under 2.0.

(2 LDL : 1 HDL) no higher than this.
BP reading to be considered hypertensive?
140/90.

But even 130 can mean increased chance for bleeding/stroke.
Which drugs for hypertensive / prehypertensive people work by lowering lipids?
STATINS.

They inhibit the rate-limiting step in cholesterol synthesis.
What drug helps prevent MI's by inhibiting platelet aggregation?
Baby apsirin
When are thrombolytic drugs used?
EMERGENCY ROOM ONLY! Given via IV for OCCLUSIVE STROKES (not bleeding strokes). Breakup a thrombus.
What drugs are used for CHF? Do they have any issues?
Digitalisglycosides

VERY low T-index (3-4). Involved in a lot of ADRs
What drug types are used for cardiac arrhythmias?
Beta blockers
Ca-channel blockers
IV Lidocaine (during fib)

*Mentioned warfarin/dicumerol, but didn't say it really treats an arrhythmia.
Sublingual nitroglycerin (Nitrostat)

How is it used? What does it do
ACUTE drug for angina attacks.

No 1st pass effect, works almost as fast as IV.
Gives off NO in blood --> stim cGMP --> vasodilate everywhere
Decreases MYO O2 DEMAND via decreasing heart workload and periph. resistance.
Name some bad characteristics of sublingual nitroglycerin.
Orthostatic / postural hypotension
Overdose: get a reflex tachycardia (bad)
Strongly oxidizing: can cause METHEMOGLOBANEMA.
Name some nitrates people take daily?
Isorbide & Erthldinitrate.

These are taken on a fixed schedule to PREVENT attacks by keeping bv's open. These are "prophylactic" nitrates.
An alternative to nitrates to take chronically for angina?
Beta blockers, they reduce myo-oxygen damand.
What is intermittent claudication?

What drugs make it worse?
People that have rigid RBCs that have trouble going through occluded blood vessels in legs. Get severe leg pain/cramps.

Beta2 blockers! Receptors here would normally vasodilate, now they can't and are constricted.
Name the uses for beta blockers
Lowers BP/CO
Fight arrhythmias
Performance anxiety
Migraine headaches - blocks the vasodilatory phase of the spasm
How will you remember ca-channel blockers used prophylactically?
the -PINES!

But the pines don't touch the heart. Only vasodilate blood vessels!

Therefore, NOT good to treat an acute attack, only prophy
What Ca-channel blockers act on both blood vessels AND the heart?
Verapamil & Diltiazem

Vasodilate bv's AND decrease HR/C.force
Baddies from taking ca-channel blockers?
Gingival hyperplasia
Orthostatic hypotension
Interaction with grapefuit / alcohol: levels of drug skyrocket (severe hypotension)

With -pines: see a REFLEX TACHY. (not as much with vera and dilt, bec they are helping heart)
What type of person takes CHF drugs?
Have had a heart attack and damaged heart muscle, you have low exercise tolerance. Without treatment your heart will FAIL in about a year.
How do CHF drugs work?
Poison/Block the Na-K-ATPase pump. (which normally pumps K in and Na out)

Block = increases Ca inside cardiac cells, increases C.FORCE
What are a secondary effects of CHF drugs that are actually a good thing?
Parasympathomimetic: prevent increases in HR

Increase fluid excretion @ kidney: helps with edemas
Tight monitoring of CHF drugs: what if drug levels too low? too high?
Low = get CHF
High = cardiac arrhythmias
Side effects and baddies of CHF drugs?
Tight tight monitoring, Tindex of 3. Need to play with dose to get it just right and monitor.

Early side effects: salivation/diarrhea/color and light sensitivity
Worst: ventricular arrythmias
Digoxin: what's a problem with this CHF drug?
10% of ppl have "eubacterium lentum": which DEACTIVATES 30% of the drug. Need to take higher dose of digoxin to have good effect.

BUT if on ANTIBIOTICS: drug levels of digoxin spike to fatal levels.
Digitoxin: what's a problem with it?
metabolized by liver more than digoxin, so it has interactions (erythromycin/barbituates..), INCREASE drug levels
What else can be used for CHF besides digoxin and digitoxin?
Loop Diuretics!! (thiazides used moreso for BP)
Fursemide. Used in addition to digitalglycosides to help with the edemas.
Problems with diuretics?
Xerostomia / gout / causes increased glucose levels (diabetes), and also excrete too much POTASSIUM.

Low potassium = v.arrhythmias, and digitalis drugs increase the risk further!
Potassium sparing diuretics?
Sporanolactone (aldosterone inhibitor)
Besides digitalis drugs and diuretics, what else for CHF??
Alpha blockers! Block a1 receptor, relax bv's.

Another use for them: men with enlarged prostates.
ACE inhibitors: what is their main use?
Lower BP.

These are the "-prils"

Blocks angio1-->2 conversion. Angio2 normally increases HR via CNS (crosses BBB)
Problem with ACE inhibitors?
They block breakdown of bradykinin (natural vasodilator), but increase bradykinin leads to unproductive cough in some people, and they hate it (might stop taking the drug).

Also cause "angioedema" - swollen face.
Angiotensin 2 receptor blockers
Do NOT block the conversion from angio1-->2. Doesn't affect bradykinin breakdown.

These are the "SARTINs" *check*

Used to lower BP!!
What drugs to use for arrhythmias?
Beta blockers
Ca-channel blockers: NOT the pines, "Veraparnil and diltazen"
Phenytoin - for ppl with epilepsy, which is kind of like an arrhythmia in the brain.
Phenytoin: uses and bad effects?
Used for arrhythmias

Gingival hyperplasia effect
Lots of sedation with it, crosses the BBB and slows e-activity.
Name some a1/b1/b2 blockers:
Carvedilol
Labetalol
What are Na-channel blockers used for?
Emergency situations:

Lidocaine
Procainamide
Amiodarone
How do erectile drugs work?
Inhibit PDE5 (phosphodiesterase5), and PDE5 normally inactivates cGMP. Leads to elevated cGMP levels --> vasodilates.
Basic q: what drug types are A-S-H?

How do they exert effects?
Benzo's and Barbs

CNS Depressants, act below the cortex (reticular activating system / limbic system.

@ high doses: will depress the cortex.
Define antianxiety
Takes the edge off, but can still talk. DON'T DRIVE though.
Define sedation
Patient is sleepy, but still have protective reflexes.
Define hypnosis
Induces SLEEP, but patient is STILL ROUSABLE.

If deep enough, you CAN lose protective reflexes.
True/False: A-S-H drugs produce some analgesia.
FALSE NO ANESTHESIA.

MUST use local or general, something with analgesic effects.
Difference between deep sedation and general anesthesia?
Deep sedation = in and out of consciousnes. General = you're OUT cold.
Problems with barbituates?
LOW Tindex
Enzyme inducers (drug interactions)
Hyperalgesic (increased pain)
What's the name of the "ultra short acting" barbituate?
Methohexital (Brevital)

- still need to use local
What are the A-S-H "others" categories?

What is their TI like?
Alcohol, Antihistamines, and Carbamates.

Alc/Carb: Ti is inbetween benzos and barbs.
How do "muscle relaxants" work?
They work on pathways from BRAIN. They do not act on muscles (like curare/dantrolene do)
How do the classic antihistamines work (the ones that make you drowsy?)
Block H1 receptors.
How antihistamines that treat ulcers/reduce GI secretion work?
Block H2 receptors
Chemical structure mods:
Phenol group on R2?
Putting lots of C's on? ("organics")
Sulfur groupos?
Phenol = enhances anti-convulsant activity
Carbons: enhances the CNS depressant effect
Sulfur = increased lipid sol (fast onset/offset)
What is thiopentyl (aka Pentohal) used for?

Bad side effect?
IV general anesthetic. As an INDUCER, before being put on volatile liquid.

Works FAST, helps get them out within 20 seconds, don't have to wait.

Hangs around lipids for a few days, get a "hangover" effect
Compare Midazolam (Versaid) to Diazapam (Valium)
Midazolam: short-lived metabolites! And WATER soluble

Diazapam: active metabolites (lasts a long time), dissolve in propylene glycol (burns on injection...'thrombophlebitis')
What are some issues with barbituates?
Coughing/hiccups after waking up

Tolerance/Abuse!, both pharmacodynamic+kinetic. Dec in post-syn receptors, and barbs induce enzymes to break themselves down

Messes up REM sleep!
What is Fiorinal?
Combo of ASA (aspirin) + Butalbital.

Treats headaches/migraines.
Withdrawal is BAD.
What's worse: withdrawal from opioids or barbituates?
BARBS. (+alcohol..)

Get opposite effect, so you see heavy seizures. Don't see this in opioid withdrawal.
Antagonist for barbituates?

What happens during overdose?
NO ANTAGONIST.

Overdose = resp depression (don't respond to increased CO2), lose protective reflexes. Ensure airway isn't blocked.
Antagonist for Benzos? *drum roll*
Flumazenil!
Methohexatol / Thiopentathol
know these..look up info
Benzo receptors:
BZ1?

BZ2?
BZ1 = sleep! Stim = sleep

BZ2 = cognition/memory/anticonvulsant activity/muscle relax (via CNS)
DEA classes:
Barbs vs Benzo?
Barbs: many are Class II

Benzos: Class IV. Can still become dependent, but not as often, and withdrawal isn't as bad (no seizures etc)
What are some Benzo Benefits!
No enzyme induction
More selective than barbs: easier to get anti-anxiety without pushing into sedation
Don't screw up REM sleep
Better at muscle-relaxation
Weird drug, and "Inverse Agonist" benzo: what's it called? What does it produce?
Beta-Carboline

BINDS to the benzo receptor, but PRODUCES anxiety and convulsions!! (does the opposite of an agonist)
When is the one time barbituates beat out benzos as a top choice drug?
Treatment of hyperthyroidism...makes epi/NE work better? (?)
Use for Clonazepam (Klonopin)?
panic attacks
Use for Triazolam (Halzion)?
"Sleep dentists" : given sublingually, works fast.

Some dentists giving too much of it, levels still rising when they leave office.
Use for Alprazolam (Xanax)?
Given to people with anxiety/depression.
How do you get tolerance from benzo?
Downregulation of post-syn receptors. (NOT from enzyme-inducing)
Pregnancy category for benzo?
D or X. BAD!

Causes cleft palates
What drugs can cause anterograde amnesia?
Benzodiazepenes
Remember: All locals can cause seizures at high enough doses!!
woot
What's a bad thing to do if you're a patient taking benzos or barbs at home?
Drink alcohol. DOUBLE DEPRESSION WHAMMY :'( :'(
Benzo structure:

What do the newer ones have?
Amidazole ring and random halogens stuck on = increases lipid sol AKA POTENCY

Also: shorter duration (less active metabolites)
Benzo structure:

What feature does Flumazenil LACK (that is responsible for activating the receptor?)
A benzene ring on the bottom
How do benzo receptors and GABA receptors interact?
Benzo's INCREASE GABA's affinity for its own receptor. Makes it WORK BETTER!

Remember: each has their own receptor on the Cl-channel. Bound = increased Cl opening freq for Cl influx --> hyperpolarized aka inhibited.
What is the receptor for alcohol and barbs?
Unknown!

Aside: Chloral Hydrate = jack daniels for kids.
What can you give to an alcoholic going through some rough withdrawal symptoms?
A-S-H drugs! Benzos or Barbs. There is CROSS TOLERANCE

Also mentioned: antihistamines have no cross tolerance.
What makes barbituates/alcohols more dangerous than benzos?

(think mechanisms)
Benzos = just increase Cl opening frequency

Barbs = Cl openings PLUS:
physically open Cl channels without GABA present
AND depress excitatory aa's (glutamate)
Is giving midazolam/triazolam safe for children?
Yes, but WATCH yourself bad things can happen. Can get resp depression (O2 saturation levels plummet)

Kids can also get "gate ataxia"

Kids also more likely to obstruct their our airway during deep sedation
Blood pressure indication for hypertension?
140/90.
Unmodifiable Risk Factors for High BP?
Genetics
Increased age
Male
African American
Diabetes
Modifiable risk factors for high BP?
High sodium (high salt = retained water, get high BP)
Losing weight lowers BP
3-5 drinks a day = increased risk
Smoking (vasoconstricts/inc HR)
Exercise/Stress
Mean Arterial Blood Pressure = ?
PVR x CO

PVR: bv diameter, type of vessel, stiffness
What drugs lower BP by lowering PVR?
Alpha 1 blockers
Ca blockers
Nitrates (in emergency situations)
Mentioned later:
Angio2 receptor antagonists / ACE inhibitors
What determines CO?

What drugs lowers BP by lowering CO?
C.force / HR / Preload

Beta blockers, and some Ca channel blockers (via HR/C.Force)
Preload lower: diuretics
3-4 General ways to lower BP:
Depress the CNS
Open the pipes (vasodilate)
Depress the pump (b-block/ca-block)
Decrease fluid volume
Name the two non-selective alpha blockers mentioned in lecture to tx high BP.

What is an undesired effect of these drugs?
phentolamine and phenoxybenzamine

Block A2 = increased NE, get reflex tachycardia
What happens when you push the dose of Epi w/ patient on an alpha blocker?
BP DECREASES

Get pure beta 2 effects. Called "epinephrine reversal"
How will you know a drug is and alpha-1 selective block?
ends in "-tocin"
Where do thiazides work? What are they used for?
Distal tubule: decrease re-ab of Na/H2O (but also decrease re-ab of potassium..can be a problem, cause arrhythmias)

Used for lowering BP. Loop diuretics = for CHF.
What is clonidine used for?
A 2nd/3rd line drug for antihypertension.

Also used to treat withdrawal from CNS depressants