The 5 main classes of drugs used to treat Heart failure are- fill in missing classes

1) Diuretics

2) Inhibitors of RAS

3)

4) Beta Blockers

5)

3) Na/K ATPase Blockers

5) Vasodilators

Fuorsemide is a loop diuretic used in the treatment of

a) mild heart failure

b) pulmonary edema

c) in patients who cannot tolerate ACE inhibitors

d) decompensating heart failure

b)

Fuorsemide is used in the treatment of pulmonary edema

Which 2 molecules does Captopril affect to decrease total peripheral resistance and dilate blood vessels to treat heart failure patients?

a) bradykinin

b)renin

c)NO

d) angiotensin II

Captopil is an ACE inhibitor that acts on A) bradykinin and D) angiotensin II

Which drug is an Angiotensin I antagonist?

a) thiazide

b) digoxin

c) hydralazine

d) metoprolol

e) losartan

e) Losartan is an AT1 antagonist.

It is potent and causes vasodilation.

What is the MOA of digoxin?

a) inhibit the Na/K pump, increasing intracellular Na and decreasing Ca expulsion

b) activating Na/K pump, increasing intracellular Na and decreasing Ca expulsion

c) inhibit the Na/K pump, decreasing intracellular Na and decreasing Ca expulsion

A

Which eventually leads to more Ca being released from the sarcoplasmic reticulum, since there is more to access in the cell.

What is hydralazine?

a) + inotrope

b) AT1 antagonist

c) ACE inhibitor

d) Vasodilator

e)beta-blocker

d)Hydralazine is a vasodilator.

Using NO to cause smooth muscle relaxation.

Hydra-LAZY-ine --> lazy=relaxation!!

Metoprolol is selective/non-selective?

Propranolol is selective/non-selective?

Which one is used for heart failure as well as antiarrythmias?

Metoprolol --> Selective for Beta 1.

Propanolol --> Non-Selective for Beta 1 and 2.

Metoprolol is used for both. since it is selective.

Match

1) Clonidine

2) Prazosin

a) Alpha 1

b) Alpha 2

Clonidine is "C"entrally acting --> it is antagonizing alpha 2 receptors in the brainstem.

Prazosine is "P"eripherally acting --> it is antagonizing alpha 1 receptors in the periperal vasculature.

both reduce PVR

Which drug lengthen the action potential by increasing the refractory period?

a) Quinidine Sulphate

b)Lidocaine

c) Verapamil

d) Amiodarone

d) amiodarone

- K+ channel blocker, slows repolarization

Which 2 drugs use NO as their mechanism of action?

a) Nitroglycerine

b)Verapamil

c)hydralazine

d)Clonidine

a) Nitroglycerine (anti-angina)

&

d) Hydralazine (vasodilator for heart failure)

Both use NO as their MOA. to reduce smooth muscle tone and cause vasodilation.

Which drug is not used for the purposes of increasing oxygen delivery to the heart during angina?

a)Nitrates

b) Beta blockers

c) Ca blockers

b) beta blockers

-this drug will decrease the oxygen demand by decreasing sympathetic input to the heart thus decreasing HR.

Heart SA and AV nodes

Cardiac muscle

Kidney - renin release

skeletal muscle BV- for dilation

bronchioles - relaxation (important for asthma)

GI tract - decreases motility in walls

Urinary tract - relaxes bladder

liver - for glucgenolysis

--sympathetic responses for fight/flight

1) Na Channel blocker (decreases excitability)

2) Beta Adrenergic blockers (decrease SNS input)

3) K Channel blocker (prolongs AP)

4) Ca Channe Blocker (decreases ability to contract)

1) Mimic ACh (receptor agonist)

2) AChase inhibitor (stop enzyme from degrading it in the synapse)

What are:

Acetylcholine

Betanechol

Carbanchol

Pilocarpine

Of the indirecting acting cholinergic receptor agonists which drug is the longer lasting one?

a) Quaternary Alcohol --edrophonium

b)Carbamate Ester - neostigmine

It is an irreversibly binding cholergic agonist --> it phosphorylates the cholinesterase and renders it inactive.

It is used for the treatment of glaucoma and causes intense miosis. It increases outflow and decreases production.

What should you give 3 year old Courtney if she starts to hallucinate in your office after you have given her Atropine drops in order to do a cycloplegic refraction?

a) Acetylcholine

b) Edrophonium

c) Physostigmine

d) Isofluorophate

c) Physostigmine

- since it enters the CNS and will reverse the parasympatholytic effects of pilocarpine.

What are characteristics (Selective/Non-Selective), (alpha/beta receptor) of:

Phentolamine

non-selective alpha receptor blocker

- used in pheochromocytoma

-due to alpha 1 block it causes vasodilation and decreases PVR and BP

Pentol - P for potent and pheochromocytoma

Amine - A for Alpha receptor blocker

What are characteristics (Selective/Non-Selective), (alpha/beta receptor) of:

Prazosin

Selective alpha receptor blocker -->Alpha 1

-it is more used since it is selective (than phentolamine)

-it also dilates BV

-for chronic HTN

What are characteristics (Selective/Non-Selective), (alpha/beta receptor) of:

Propanolol

Non-selective

B1 and B1 blocker

for HTN, angina, arrthmia

What are characteristics (Selective/Non-Selective), (alpha/beta receptor) of:

Timolol

non-selective beta blocker

-used to decrease IOP in glaucoma since there are beta receptors on the ciliary epithelium -- blocking that would decrease production of AqH

What does "negative inotrope" mean and what kind of drug does this?

What does "positive inotrope" mean and what kind of drug does this?

Negative inotrope means to decrease the heart beat strength. In the Adrenergic Receptor Anatagonist lecture: Metaprolol does this.

Positive inotrope means to increase the strength of the heart beat. In the Heart Failure lecture: Digoxin increases the strength (a Na/K Blocker)

RESIN!! It prevents reabsorption of cholesterol and increases clearance.

Statins are the most used hyperlipidemia drug

Which 2 are pro-drugs? (the others are active drugs)

a) Lovastatin

b)Fluvastatin

c)Simavastatin

d) Atorastatin

e)Pravastatin

Lova and simava --statin

They inhibit

HMG-CoA reductase --involved in the synthesis of cholesterol.

this decreases LDL in serum, increases LDL in hepatocytes which increases clearance.

Which class of hyperlipidemia drug do you need to monitor clotting time due to an increase in warfarin?

a) Resin

b) Statin

c) VLDL secretion inhibitors

d)Lipoprotein Lipase Stimulants (fibrates)

e) Inhibition of Intestinal Sterol Absorption

Which vitamin is a VLDL secretion inhibitor used in hyperlipidemia?

a) B12

b) Iron

c) Niacin

d) Folic Acid

c) Niacin

When you take Niacin you also need to take aspirin to prevent the prostaglandin release from causing urticaria and itching.

Rudolf has a familial hyperlipidemia disease for which he takes Gemfibrozil. Which lipoprotein does this act on?

a) HDL

b)LDL

c) IDL

d)VLDL

Inhibitor of intestinal sterol absorption

-targets transport protein NPC1L1 so cholesterol and phytosterols are not absorbed in the first place.

After there is damage to the blood vessel wall what are the 2 components that begin the clot formation process?

1) Platelet component --> platelet is exposed to collagen and becomes activated. It releases other meidators and recruits more platelets to form aggregating mass.

2) Formation of Thrombin --> key player in converting fibrinogen to fibrin.

These both lead to the formation of the thrombus whcih is made of fibrin and platelets.

Extrinsic factors come from ...

Intrinsic factors come from ...

Extrinsic --from tissues

Intrinsic --from plasma

Donepezil

"Donzies with Alzheimer's"

It is an acetyl-cholinesterase inhibitor: inhibiting the enzyme that breaks down ACh.

1) Dopamine Agonist --L-Dopa

2) MAO inhibitor -- selegiline

3)Anti-muscarinic --benztropine

Anti-muscarinic -- Benzotropine.

since it decreaes activity of cholinergic neurons in basal ganglia.

Typical Neuroleptics cause more of what kind of symptoms?

Atypical Neurleptics cause more of what kind of symptoms?

Typical --> movement disorders

Atypical --> Weight gain, increased negative sxs

Tricyclic Antidepressants

--selective amine reuptake inhibitors

--it affects NE and serotonin

2nd-3rd generation Amine reuptake inhibitior -- selective for dopamine.

Has less sedative and autonomic side effects than trycyclics.

Fluoxetine 

(PROZAC)

Phil is depressed and fluoxetine is not working. His doc decides to put him on Phenelzine. What is that?

One day Phil decides to eat some feta cheese, what should he be worried about?

Phenelzine is a Monoamine Oxidase Inhibitor.

Phil should worry about a hypertensive crisis, since he ate tyramine-containing food. this causes even more norepinephrine syntehsis, so there is way to many NT being active in the synapse.

PIP2 resynthesis.

And protein kinase C.

Benzo drugs like Diazepam requires GABA to be bound to the receptor for increased activation.

Barbiturate drugs like Phenobarbitol and Pentobarbitol at HIGH doses can activate GABA receptor without GABA being present.

(both increase opening of Cl- channel, more suppression of neurons in brain) to treat anxiety.

65 year old Ron comes in to your office and he informs you he is on Prazosin. What should you be wary of during the exam?

a) his blood pressure may get too high

b) if he gets up too fast

c) the dilation drops will react with it

d) if his heart rate gets too low

b) if he gets up too fast he could faint!!

Tachycardia and syncope upon getting up are side effects

Clonidine is a alpha 2 agonist, what are its pharmacological effects?

a) sympathomimetic effects - increased BP

b) sympatholytc effects - decreased BP

KT has asthma, which drug should you not give her because of this information?

a) Metoprolol

a) Nitroglycerine

c) Propanolol

d) Hydralazine

c) Propanolol -- it is non-selective antagonist for Beta 1 and 2 --> thus it affects the bronchioles! You don't want to make the asthma worse by constricting the bronchioles via Beta 2.

Metaprolol is safe since it is selective for Beta1

timolol

You are diagnosed with Schizophrenia and you are deciding between typical and atypical neuropeltic drugs. You decide that you would rather have parkinsonian symptoms than gain weight or lose pleasure/cognition. Which drug did you choose?

a) Phenothiazine

b) Clozapine

c) Selegiline

d) Benztropine

a) Phenothiazine

Clozapine makes you gain weight and increases negative symptoms.

C and D are for treating Parkinsons.

Identify the false statement about Lidocaine

a) binds to g-protein coupled receptor

b) blocks voltage sensitive Na channel

c) often combined with "epi"

d) amino compound metabolized by hepatic p450

What is the most potent opioid on our drug list?

a) Morphine

b) Meperidine

c) Fentanyl

d) Oxycodone

c) Fentanyl --100x more potent

Rapid onset, short duration of action. Used for profound pain. Given IM or as a controlled patch

Which type of GPCR is present at both the pre and post synaptic membrane?

a) Mu

b) Kappa

c) Delta

d) Gamma

a) Mu

it closes voltage gated Ca channels to reduce NT release on pre-synaptic membrane. It keeps the K channel open on the post-synaptic membrane to create hyperpolarization.

(gamma is not one)

When you give a mother an opioid for delivery, why do you need to worry about the baby?

a) the baby is small, higher drug concentration

b) the baby cannot metabolize it

c) the baby has more GPCRs

d) you don't need to worry it doesn't cross the placenta

b) the baby cannot metabolize it.

Opioids are metabolised in adults to inactive glucuronide conjugates to be excreted. Babies cannot do this conjugation.

Classify these glucocorticoids as short/medium/long acting

Triamcinolone, Prednisone, Dexamethasone

Prednisone -- short acting

Triamcinolone -- medium acting

Dexamethasone -- long acting (used for septic shock and brain edema)

All three have low mineralocorticoid activity.

What is not one of the recommendations for dosage of glucocorticoids?

a) alternate day therapy

b) use low doses

c) ensure the full course is taken

d) apply locally if indicated

True - topical preparations.

For things like uveitis and allergic conjunctivitis.

Other uses:

GI disease, infections (septicemia), bone/joint disease, lung disease, skin disease, allergic reactions.

Glucorticoid MOA:

a) bind to GPCR

b) binds to COX-1

c) binds to DNA response elements

d) binds COX-1 and COX-2

c) binds to DNA response elements to affect the genes involved in inflammation

(WBC suppression and inhibition of Phospholipase A)

Aspirin irreversibly binds COX-1 and COX-2, which inflammatory product is unaffected by this:

a) Prostaglandins

b)Thromboxanes

c) Leukotrienes

d) Bradykinin

Who is safe to take aspirin?

a) 5 year old warren with a high fever

b) 40 year old bob with hemophilia

c) 80 year old edna with kidney failure

d) 20 year old KT with asthma

e) none of the above

f) all the above

Martha has rheumatoid arthritis and needs a chronic pain medication. What is the best choice for her?

a) Aspirin

b) Celebrex

c) Acetaminophen

d)Oxycodone

b) Celebrex

-selective COX-2 inhibitor, that affects the inflammatory synthesis of prostaglandins but not the constitutive COX-1 effects. Thus no bleeding risks, less renal toxicity, reduced GI toxicity.

Acetaminphen --no anti-inflammatory effects, thus useless for RA. Aspirin/oxycodone have too many side effects for chronic use.

Which anti-inflammatory drug requires proper enzyme function in order to eliminate?

a) aspirin

b) celcoxib

c) acetaminophen

c) acetaminophen does.

Without enzmes to add glucuronate or sulphate to the acetaminophen, P450 hepatic enzymes take over and make reactive electrophilic compounds that cause liver failure.

Which drugs are used for treating the acute early response symptoms of asthma?

a) Albuterol

b) Ipratropium

c) Aminophylline

d) Chromolyn

e) Glucocorticoids

the beta agonists and aminophylline.

A and C.

Ipratropium (M-antagonist) is more used for chronic treatment of COPD, since it can treat the late response (inflammation, bronchial hyperactivitiy).

Chromolyn is a release inhibitor that is used as a prophylaxis for asthma.

Which beta agonist is longer acting?

a) abuterol

b) salmeterol

Isofluorophate is an indirect cholinergic. It blocks AChase thus allowing ACh to active in the synapse longer. This activates the M receptors on the sphicter and ciliary body causing miosis and CB contraction.

Contraction of the CB increases AqH outflow thus allowing IOP to drop.

What is tropicamide and how does it affect the eye?

Systemic administration of what, causes bradycardia

a) dopamien

b) epinephrine

c) prazosin

d) pilocarpine

e) tropicamide

Epinephrine is often used with local anesthetics, why is that?

a) speeds absorption

b) epinephrine delays absorption of anesthetic

c) decreases intensity and delays activity of anesthetic

d) does nothing to intensity but it increases anesthetic activity

e) epinephrine has local anesthetic properties

b) it delays absorption of anesthetic

--epi is is a direct receptor agonist of all subtypes. Thus there is vasoconstriction of BV -- making it harder for drug to diffuse away thus making it have longer effects in the area you want.

Which drug does not produce either direct or indirec parasympathomimetic effects?

a) bethanechol

b) neostigmine

c) edrophonium

d) atropine

e) pilocarpine

Atropine overdose does not cause

a) blurry visiion

b) decreased saliva

c) decreased gastric secretion

d) mydriasis

e) decrease HR

What does not occur in decompensated heart failure?

a) pulmonary edema

b) increased RAS activity

c) tachycardia

d) cardiomegaly

e) hypotension