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Pharm 2 Mod 2
.
126
Pharmacology
Graduate
10/15/2009

Additional Pharmacology Flashcards

 


 

Cards

Term
3 determinates of myocardial O2 demand
Definition

HR

Myocardial contractility

Intra-myocardial wall tension

Term
Drug of choice for chronic stable angina?
Definition
B-blockers
Term
What drugs increase coronary blood flow?
Definition
Nitrates, CCBs
Term
What drugs improve regional blood flow distribution?
Definition
Nitrates, CCBs & B-blockers
Term
What drugs decrease HR & cardiac contractility?
Definition
B-blockers & some CCBs
Term
What drugs decrease myocardial wall tension? How?
Definition

Nitrates- decrease preload

CCBs- decrease afterload

Term
What is nitric oxide physiologically identical to?
Definition
EDRF- endothelium-derived relaxation factor
Term
Actions of NTG
Definition
Venodilation and coronary artery dilation
Term
Important pharmacokinetics of NTG
Definition
1st pass effect & low bioavailability
Term
Major drug interactions of NTG
Definition
Erectile dysfunction drugs
Term
Usual dose of sublingual NTG?
Definition
0.4mg
Term
This drug has the same pharmacological activity, SE and drug interactions as NTG, but has a slower onset and longer duration. Active metabolite?
Definition

Isosorbide dinitrate (Isordil)

AM: Isosorbide mononitrate

Term
Active metabolite of isosorbide dinitrate, has 100% bioavailability
Definition
Isosorbide mononitrate (Imdur, Monoket)
Term
Non-DHP CCBs work on which type of calcium channels?
Definition
L-type Ca channels
Term
Physiological effects of non-DP CCBs
Definition
Vascular smooth muscle relaxation: reduces BP, wall tension & CA vasospasm
Term
What is the "prototype" DHP-CCB?
Definition
Nifedipine
Term
DHP-CCB with the longest T1/2?
Definition
Amlodipine (T1/2 = 40h)
Term
SE and contraindications of DHP-CCB use.
Definition

SE: Peripheral edema, flushing, headache

C: Heart failure

Term
SE & contraindications of verapamil
Definition

SE: Same as DHP-CCBs + bradycardia & constipation

C: LV dysfunction & heart failure

*Dilitazem does not cause constipation

Term
Which B-blockers are commonly used for chronic stable angina?
Definition

Cardioselective: Atenolol & Metoprolol

Non-cardioselective: Nadolol & Propanolol

Term
10-Point plan for Chronic Stable Angina (ABCDE)
Definition

A: Aspirin & antiplatelets

B: B-blockers and BP

C: Cholesterol & cigarettes

D: Diet & diabetes

E: Education & exercise

Term
What type of anti-ischemic drug should be administered w/in 24h if a patient presents with Class I unstable angina?
Definition
B-blocker
Term
What type of anti-ischemic drug should be administered w/in 24h if a patient presents with Class III unstable angina?
Definition
Nitrates
Term
In preparation for a CABG, what drug must be withheld for 7 days prior?
Definition
Clopidogrel (Plavix)
Term
What anti-platelet drug should be administered asap if a pt presents with Class I unstable angina?
Definition
Aspirin
Term
Which two classes of anti-arrhythmic agents slow ventricular response?
Definition
Classes II and IV
Term
Which class of anti-arrhythmic agents is not effective against supraventricular arrhythmias?
Definition
Class Ib
Term
What are the common types of supraventricular arrhythmias?
Definition
Asystole, PEA, sinus bradycardia, paroxysmal supraventricular tachycardia, atrial flutter, a-fib
Term
Management strategies of A-fib
Definition

1. Ventricular rate control

OR

2. Conversion to and maintenance of normal sinus rhythm

PLUS

3. Thromboembolism prevention

Term
According to the RACE trial results, does rate control or electrical cardioversion result in less side effects?
Definition
"Adverse effects less with rate control agents"
Term
What are some agents for heart rate control in A-fib?
Definition

- B-blockers: Metoprolol, propanolol, esmolol

- Non-DHP CCBs: diltiazem, verapamil

- Digoxin

Term
Most effective drug class for rate control of A-fib?
Definition
B-blockers (Class II)
Term
Major drug interactions of CCBs
Definition

Digoxin: Inc concentrations

CYP-3A4 inhibitors

Term
Contraindications of CCB use
Definition
Heart failure, WPW
Term
Preferred A-fib rate control drug if the patient is in heart failure or  has LV dysfunction?
Definition
Digoxin
Term
High-dose SE of digoxin?
Definition
AV block & ventricular tachyarrhythmias
Term
Major contraindication of digoxin?
Definition
WPW
Term

First-line agent for most A-fib pts requiring rhythm control and the anti-arrhythmic agent of choice in heart failure.

EKG changes associated with this drug?

Definition

Amiodarone

Prolonged QT interval

Term
Class III agents for sinus rhythm control in A-fib
Definition
Amiodarone, sotalol, dofetilide (Tikosyn)
Term
Class Ic agents for sinus rhythm control in A-fib
Definition

Flecainide (Tambocor)

Propafenone (Rhythmol)

Term
Amiodarone is used in patients with _______________, ____________ and to _______________________________.
Definition

Sustained V-tach

V-fib

Maintain sinus rhythm in A-fib

Term
SE of Amiodarone?
Definition

Pulmonary toxicity

Hyper/hypothyriod: b/c of iodine

Liver toxicity

GI: nausea, constipation

Ocular: deposits, neuritis

Derm: photosensitivity, bluish discoloration

Neurologic: ataxia, parasthesias, tremor

CV: bradycardia, heart block, torsades

Term
Drug interactions of Amiodarone
Definition

Warfarin- dec warfarin dose

Digoxin- doubles Ami levels

B-blockers, CCBs, anti-arrhythmics

Term
Structurally related to Amiodarone, this drug is FDA approved for patients with a-fib/flutter who do not have heart failure.
Definition

Dronedarone

*Doesn't contain iodine, shorter T1/2, less drug interactions

Term
The only Class III agent for both conversion and maintenance of sinus rhythm in A-fib. SE?
Definition

Dofetilide (Tikosyn) [Class III]

SE: QT prolongation, torsades

Term
Drug interactions of Dofetilide (Tikosyn)
Definition
Verapamil, cimetidine, ketoconazole, trimethoprim, prochlorperazine & megestrol all increase serum levels of Dofetilide (Tikosyn)
Term
Major benefit of using Class Ic anti-arrhythmics for a-fib
Definition
Class Ic anti-arrhythmics have a great effect of the conduction rate throughout the heart
Term
SE of Flecainide (Tambocor)? [Class Ic]
Definition

Flecainide (Tambocor) can cause:

Inc ventricular rate, dizziness (30%), visual changes, dyspnea

Term
SE of Propafenone (Rhythmol) [Class Ic]
Definition

Propafenone (Rhythmol) can cause:

Bradycardia, heart block, heart failure, nausea, taste changes, bronchospasm, constipation

Term
This drug exhibits non-linear kinetics, and serum levels may increase 10x as the dose is slowly increased.
Definition
Propafenone (Rhythmol)
Term

What is the "pill-in-the-pocket" dose of:

Flecainide (Tambocor)?

Propafenone (Rhythmol)?

Definition

 

Flecainide (Tambocor): 300mg after onset of palpitations

Propafenone (Rhythmol): 600mg after onset of palpitations

 

Term
In what patients should rate control be the first line of treatment for persistent A-fib?
Definition

>65 yo

CAD

Anti-arrhythmic drug contraindications

Unsuitable for cardioversion

Pts w/o heart failure

Term
In what pts should rhythm control be the first line of treatment for persistent A-fib?
Definition

Pts asymptomatic after rate control

< 65 yo

1st presentation w/ lone a-fib

Hypotension or worsening heart failure

Term
What is the CHADS scoring?
Definition

C: CHF

H: HTN

A: Age >75 yo

D: DM

S: Stroke/TIA

Score >2: high risk

Term
This drug is used for paroxysmal supraventricular tachcardia
Definition

Adenosine

*T1/2 = 5 seconds

Term
Class Ia anti-arrhythmic with the SEs of diarrhea and cinchonism w/ high doses.
Definition
Quinidine
Term
Class Ia anti-arrhythmic with the SE of SLE, hypotension & torsades
Definition
Procinamide
Term
Class Ia anti-arrhythmic with the SE of urinary retention, blurred vision and torsades
Definition
Disopyramide
Term
3 Class Ia anti-arrhythmic agents
Definition
Quinidine, procinamide, disopyramide
Term
2 Class Ib anti-arrhythmic agents
Definition
Lidocaine, Mexiletine (Mexitil)
Term

This anti-arrhythmic agent is only available IV for treating ventricular arrhythmias.

Major SE?

Definition

Lidocaine

SE: Tremor, hallucinations, & parasthesias  (w/ high serum levels)

*Mexiletine is oral

Term
What type of anti-arrhythmic drugs may result in Torsade de Pointes?
Definition
Drugs that prolong the QT interval
Term
How is Torsade de Pointes treated?
Definition
IV magnesium sulfate or isoproterenol
Term
Drug tx of mild to moderate migraine attacks?
Definition
NSAIDs, analgesics w/ caffeine
Term
4 Therapeutic strategies for migraine headache treatment
Definition

Abortive

Analgesic

Anti-emetic

Prophylactic

Term
Most prescribed -triptan for migranes
Definition
Sumatriptan
Term
SE of sumatriptan (Imitrex)
Definition

Coronary vasocontstriction

(contraindicated in CAD or uncontrolled HTN)

Tingling, flushing, dizziness

Term
These two -triptans have a longer T1/2 an duration of action than sumatriptan.
Definition

Naratriptan (T1/2: 6h)

Frovatriptan (T1/2: 26h)

Term
Preferred ergot alkaloid for tx of migraines?
Definition
Dihydroergotamine mesylate (DHE)
Term
SE of ergot alkaloids?
Definition

Nausea & vomiting (give anti-emetic, ie metoclopramide)

Ergotism (gangrene)

Uterine contractions: pregnancy X

Term
How does a pt prevent medication overuse headache?
Definition
Limit use of ergots, triptans and analgesics to 10 days per month
Term
What are the first line drugs for migraine prophylaxis?
Definition

Beta-blockers: propanolol & timolol

Tricyclic antidepressants: amitriptyline, nortriptyline

Valproic acid derivatives: depakote & depakene

Topiramate

 

Term
Tx of migraines in children?
Definition

NSAIDs, nasal spray sumatriptan

Prophylactic: propanolol

Term
Most common type of primary headache?
Definition
Tension-type
Term
Antiepileptic drugs block which type of calcium channels?
Definition
T-type
Term
What are some basic principles of anti-epileptic therapy?
Definition

- Drug choice is based on seizure classification

-Monotherapy preferred

-Least-sedating agents

-Least drug interactions

Term
Which anti-epileptic drugs are most sedating?
Definition

Phenobarbital

Primidone

Benoziadepines

Term
Drugs of choice for partial seizures?
Definition

Carbamazepine

Phenytoin

Oxacarbazepine

Gabapentin*

Lamotrigine*

Topiramate*

 

Term
Drugs of choice for generalized tonic-clonic seizures?
Definition

Valproate

Phenytoin

Carbamazepine

Lamotrigine*

Topiramate*

 

Term
Drugs of choice for generalized absence seizures?
Definition

Ethosuximide

Valproate

Lamotrigine*

 

Term
Drugs of choice for myclonic, atonic & atypical absence seizures?
Definition

Valproate

Lamotrigine

 

Term
This anti-epileptic drug undergoes autoinduction, resulting in a decreased T1/2 over the first month of use.
Definition
Carbamazepine (Tegretol)
Term
SE of carbamazepine?
Definition

Leukopenia (monitor WBCs every 2wks for 1st month)

Rash

SLE

Aplastic anemia

 SIADH

Term
What CYP enzymes are affected by carbamazepine? How?
Definition
Carbamazepine induces 2C9, 2C19 and 3A4
Term
What seizure types are treated with carbamazepine?
Definition

Partial and generalized T-C

* Aggravates absence & myclonic

Term
What seizure types are treated with Phenytoin (Dilantin) and Fosphenytoin (Cerebyx)?
Definition

Partial and secondarily generalized seizures

*Aggravates absence seizures

Term
What are the notable kinetics of phenytoin?
Definition

Zero-order kinetics at higher doses b/c of saturation

Narrow therapeutic range

Must adjust dosage for low albumin levels

Term
SE of phenytoin & fosphenytoin?
Definition
Nystagmus, dyskinesias, gingival hyperplasia
Term
These drugs are used in all types of seizures.
Definition
Valproate: Depakene & depakote
Term

SE of valproate?

Drug interactions?

Definition

SE: Weight gain, alopecia, hepatotoxicity, thrombocytopenia

DI: Warfarin, phenytoin, carbamazepine

Term
Monitoring of valproate?
Definition
Liver fxn tests & platelet count every month for 1st 2 months
Term
What seizure types are treated with phenobarbital?
Definition
Partial and generalized T-C
Term
Half life and SE of phenobarbital?
Definition

T1/2 = 100h (need loading dose)

SE: Sedation, rash, nystagmus, dizziness

Very CHEAP, $4/mo

Term

What seizure types are treated with Ethosuximide (Zarontin)? 

Effect on CYP-450?

Definition

Ethosuximide (Zarontin):

Absence seizures

NO EFFECT on CYP-450

Term

What seizure types are treated with Topiramate (Topamax)?

SE?

Definition

 Topiramate (Topamax):

Partial and generalized T-C seizures

SE: Paresthesias, decreased sweating, hyperthermia, kidney stones, metabolic acidosis

Term
Drug interactions, monitoring, and other uses of Topiramate (Topamax).
Definition

Topiramate (Topamax):

DI: Phenytoin, oral contraceptives

M: serum bicarb

Other uses: migraine prophylaxis, neuropathic pain

Term
A carbamazepine analog used to treat partial seizures that does not undergo auto-induction.
Definition
Oxcarbazepine (Trileptal) does not undergo auto-induction
Term
SE of Oxcarbazepine (Trileptal)?
Definition

Oxcarbazepine (Trileptal):

Rash, hyponatremia

Term

What seizure types are treated with Lamotrigine (Lamictal)?

SE? DI?

Definition

Lamotrigine (Lamictal):

Partial and generalized seizures

SE: Severe rash which may progress to Stevens-Johnson Syndrome

DI: Valproate

*Expensive

Term
SE: Non-convulsive status epilepticus
Definition
Tiagabine (Gabitril)
Term
Similar to Topiramate, SE: Stevens-Johnson Syndrome
Definition
Zonisamide (Zonegran)
Term
This drug is used as adjunct therapy for drug-resistant seizures only. 
Definition
Felbamate (Felbatol)
Term
SE: Aplastic anemia, acute hepatic failure
Definition

Felbamate (Felbatol)

 

Term
Types of benzodiazepines used for the tx of seizures.
Definition

Diazepam (Valium)

Clonazepam (Klonopin)

Clorazepate (Tranxene)

Term
Ideally, how long before pregnancy should AEDs be stopped?
Definition
6 months
Term
What supplements should a pregnant woman take if she continues her AEDs during pregnancy?
Definition
Folic acid, Vitamin K
Term
Drugs of choice for the tx of status epilepticus?
Definition
Diazepam or lorazepam
Term
Why is dopamine not an effective drug for the tx of Parkinson's?
Definition
Dopamine cannot cross the BBB
Term
What drug must be given with levodopa? Why?
Definition
Carbidopa b/c it blocks levodopa activity in the peripheral tissues, allowing more levodopa to act on the brain. Also prevents nausea.
Term
Why must levodopa be given on an empty stomach?
Definition
Levodopa must be given on an empty stomach to avoid absorption inhibition by proteins.
Term
Most effective treatment for Parkinson's disease?
Definition

Levodopa

is the most effective treatment for Parkinson's disease

Term
SE of Levodopa
Definition

GI: Nausea, anorexia, body fluid darkening

CV: orthostatic hypotension, inc homocystine

Neuro: sedation, hallucinations, pathologic gambling

Motor: fluctuations in motor activity, dyskinesias

Term
Major DI of levodopa?
Definition
Vitamin B6, ferrous sulfate, TCAs, metoclopramide
Term

These drugs help to metabolize levodopa in the GI tract, and increase its T1/2 by 50%.

SE?

Definition

COMT inhibitor: Entacapone

SE: Nausea, diarrhea, urine discoloration

Term

2 non-ergot dopamine agonists for the tx of Parkinson's.

SE?

Definition

Pramipexole (Mirapex)

Ropinirole (Requip)

SE: othostatic hypotension, sleep attacks, hallucinations, psychosis

Term
This drug is the only injectable drug for Parkinson's, the most potent dopamine agonist, and must be given with an anti-emetic.
Definition
Apomorphine (Apokin)
Term

This MAOBI is metabolized to L-methamphetamine

and L-amphetamine.

Definition
Selegiline
Term
Preferred MAOBI for the tx of Parkinson's? Why?
Definition

Rasagiline

*Similar to selegiline but not metabolized to amphetamines (less stimulating)

Term
SE: Livedo reticulatis (purple, mottled, fishnet-like rash)
Definition
Amantadine
Term
Anticholinergic drugs used for the tx of Parkinson's? Action?
Definition

Benztropine (Cogentin) and Trihexyphenidyl (Artane)

Balances cholinergic & dopaminergic neurotransmitters

Term
Drug therapy for essential tremor?
Definition
B-blockers: Propanolol
Term
First-line pharmacologic agents for the tx of restless legs syndrome?
Definition

Ropinirole (Requip)

Levodopa

Pramipexole

Term
4 Cholinesterase inhibitor drugs used for the tx of Alzheimer's?
Definition

Tacrine (Cognex)

Donepezil (Aricept)

Rivastigmine (Exelon)

Galantamine (Razadyne)

Term
SE of cholinesterase inhibitors
Definition
nausea, diarrhea, incontinence, insomnia, headache
Term
Most hepatotoxic cholinesterase inhibitor?
Definition

Tacrine (Cognex)

*Inconvenient: must take 4x day b/w meals

Term
Why is Riviastigmine (Exelon) an inconvenient tx for Alzheimer's?
Definition
Dose must be titrated up every 2 weeks. If a dose is missed, one must gradually taper back up to the necessary dose.
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