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Flashcards in Exam 1 Questions Deck (62):
1

Drug that inhibits AChE. Causes ACh to accumulate in the synaptic cleft.

Neostigmine

2

Drug that inhibits ACh release from vesicles; Prevents fusion of proteins with vesicle.

Botulinum Toxin

3

Drug that blocks release of NE from vesicle

Guanethidine

4

Drug that blocks vesicle uptake B and depletes NE

Reserpine

5

Drugs that block Uptake 1, causing NE to accumulate in the synase

Cocaine and Tricyclic Antidepressants

6

Drug that releases NE from vesicles into synapse

Amphetamine

7

Enzyme that deactivates NE in nerve terminals. Also found in liver and kidney

MAO: Monoamine Oxidase

8

Enzyme that is the principal extra-neuronal enzyme that deactivates NE

COMT: Catechol-o-methyltransferase

9

Muscarinic Agonists

Eye: Contract iris sphincter (miosis); Contract ciliary muscle (accommodation); Facilitate output of aqueous humor, Decrease Intra-ocular pressure. Indicated for certain types of glaucoma.
GI: Increase Secretory and motor activity. Indicated for non-obstructive, post-op ileus and severe dry mouth
GU: Stimulate detrusor and relax sphincters to cause micturition (voiding). Indicated for post surgery or post partum urinary retention
Expected Side Effects: Salivation, lacrimation, urination, defecation (SLUD); abdominal cramps, other secretions (sweating, nasopharyngeal, etc), bronchoconstriction, **DECREASED CARDIAC OUTPUT AND BP**

10

Donepezil (Aricept)

One of the four AChE Inhibitors approved for treatment of mild to moderate Alzheimers. Increases remaining cholinergic activity to partially restore function

11

AChE Inhibitors


Prototype: Neostigmine (Prostigmin)
Eye, GI, GU: Same as Muscarinic Agonists
Skeletal Muscle: Indicated for Myasthenia Gravis
Used to reverse actions of Non-Depolarizing Neuromuscular Relaxants (Tubocurarine, a Nm Receptor Antagonist)
Indicated to treat Alzheimers
Side Effects: SLUD, Muscle Spasms from therapeutic doses, Can produce paralysis of ganglia and NMJ transmission at high doses, Derivatives that penetrate CNS could exacerbate or induce Parkinsons, alertness proceeding to generalized convulsions, coma

12

Nicotine Products (Smoking Cessation)

Mechanism: Activate nicotinic receptors in brain
Adverse Effects: Nausea/vomiting, dizziness, weakness, irregular heartbeat, drug interactions

13

Muscarinic Antagonists (Atropine and Scopolamine)

Indications: Parkinsonism, Motion sickness, Peptic Ulcers, Hyper-motility, COPD, Pupil Dilation (optic exams)
Side Effects: Dry mouth, fever (inhibition of sweating), dry eyes, blurred vision, urinary retention, constipation, tachycardia, confusion, disorientation, delirium
Rehab Considerations: Exercise will add to hyperthermia and tachycardia effects... pronounced hyperthermia will further increase heart rate: potential for serious cardiac events

14

Nm receptor antagonist. Used during surgery to relax skeletal muscle.

Tubocurarine

15

Natural alkaloids found in atropa belladonna and hyoscyamus niger. Prototypes of competitive muscarinic recepter antagonists

Atropine and Scopolamine

16

A muscarinic antagonist with a functional specificity for bladder receptors. Used to treat enuresis and urge incontinence (overactive bladder)

Oxybutynin (Ditropan)

17

Muscarinic antagonist that causes bronchodilation and decreases secretions; indicated for asthma and COPD

Tiotropium (Spiriva)

18

Alpha 1 Receptors

-- Most vascular smooth muscle: Contraction; Increase TPR and venous return
-- Radial Muscle/Iris: Contraction; Mydriasis

19

Alpha 2 Receptors

--CNS: Decrease BP or cause sedation (brainstem); Decrease spasticity (spinal cord); Modify pain response (spinal cord)
-- Adrenergic and Cholinergic Nerve Endings: Inhibit transmitter release

20

Beta 1 Receptors

-- Heart (SA, AV Nodes and Ventricles): Increase HR (+ chronotropic), increase conduction ( + dromotropic), increased contractility ( + inotropic)
-- Kidney: Increase renin release

21

Beta 2 Receptors

-- Bronchioles: Relaxation (Bronchodilation)
-- Vascular Smooth Muscle (Skeletal Muscle Beds): Relaxation (Decrease TPR)

22

Prototype Alpha-1 Agonist ; Indicated for low BP, nasal and middle ear congestion; ORAL ADMINISTRATION PREFERED

Phenylephrine (PE)

23

Prototype for Non-Specific Adrenergic Agonist; Used as an adjunct for local anesthesia, for treatment of shock (Physiological histamine antagonist) and bronchial asthma; NOT EFFECTIVE ORALLY

Epinephrine

24

Releases endogenous catecholamines plus nonspecific agonist actions mimic EPI in spectrum

Ephedrine

25

Vasoconstrictor Factors

Angiotensin II, Endothelin

26

Vasodilation Factors

Nitric Oxide, Bradykinin, Prostaglandin I2

27

Presynaptic Adrenergic Inhibitors: Drugs which deplete NE by interfering with neuronal vesicular storage mechanisms

Reserpine (Serpasil); Guanethidine (Ismelin)

28

Central Alpha-2 Agonists: Centrally Acting Agents: Drugs which inhibit the medullary vasomotor center and decrease adrenergic outflow from the CNS

Alpha-Methyldopa (Aldomet); Clonidine (Catapres)

29

Beta Receptor Antagonists: Drugs that act by reducing cardiac output and renin release

Propranolol (Inderal); Metoprolol (Lopressor)

30

Drugs which decrease vascular tone by blocking Alpha-1 Receptors

Prazosin (Minipress)

31

Nonselective or Dual Alpha and Beta Receptor Antagonists: Effective for hypertensive emergencies; congestive heart failure

Labetalol (Normodyne); Carvedilol (Coreg)

32

Vasodilator: Arterial Dilation > Venous Dilation

Hydralazine (Apresoline), Minoxidil (Loniten)

33

Vasodilator: Arterial and Venous Dilation

Nitroprusside (Nipride)

34

Vasodilator: Calcium Channel Blockers

Nifedipine (Procardia XL) and Amlodipine (Norvasc)

35

Vasodilator: Endothelin Receptor Antagonists

Bosentan (Tracleer)

36

Vasodilator: Phosphodiesterase (PDE) Type 5 Inhibitor

Tadalafil (Adcirca)

37

ACE Inhibitors

Captopril (Capoten) and Lisinopril (Prinivil, Zestril)

38

Angiotensin II receptor Antagonist

Losartan (Cozaar) and Valsartan (diovan)

39

Direct Renin Inhibitor

Aliskiren (Tekturna)

40

Diuretics

Thiazides: Hydrocholorthiazine (hydrodiuril)
"Loop": Furosemide (Lasix)
Potassium Sparing

41

Ventricular Systolic Pressure

AFTERLOAD: Pressure heart must generate to overcome arterial pressure

42

Ventricular Volume

PRELOAD: Volume heart must contract against to eject blood

43

Determinants of Myocardial Oxygen Supply

Coronary Blood Flow; Diastolic Filling Time

44

Determinants of Myocardial Oxygen Demand

Heart Rate; Contractility; Ventricular Systolic Pressure (After load); Ventricular Volume (Pre Load)

45

What does the ratio of ionized to nonionized drug depend on?

-pH of the aqueous solution
-pKa of the weak electrolyte
(pKa: Index of drug's degree of ionization)

46

General Characteristics of Drug Reservoirs

-Bound drug is in equilibrium with free drug; the association is usually freely reversible
- Reservoirs may prolong drug action
-Reservoirs serve to concentrate drug in a compartment while limiting the amount of free drug
-Only FREE DRUGS can cross membranes

47

What is the goal of drug metabolism?

To convert drug molecules to inactive compounds (metabolites) which can be more rapidly excreted from body

48

Inhibitors of CP450 oxidation

- Cimetidine
-Erythromycin
-Grapefruit
(Drug levels of affected drug may rise; Increased therapeutic effect or toxicity)

49

Inducers of CP450 Oxidation

- Increase synthesis of CYP450 enzymes
-Increase rate of drug metabolism for any drug that shares its CYP450 pathway
-Decreased drug levels and drug effect
- Also increases its own rate of metabolism, an example of drug disposition tolerance

-Tobacco smoke
-charbroiled meat
-ethanol

50

Bioavailability

Fraction of unchanged drug that reaches the systemic circulation after administration and becomes available to its site of action. Determined by the measurement of the rate and extent of drug absorption after administration of a specific dosage form. Use area under the curve.

51

Daily Aspirin

- Decreases incidence of MI in MEN
- Decreases incidence of stroke in WOMEN

52

Muscarinic receptor antagonist that is prescribed in combination for traveler's diarrhea

Lomotil

53

Muscarinic antagonist with a functional specificity for bladder receptors. used to treat enuresis and urge incontinence (overactive bladder)

Oxybutynin (Ditropan)

54

Muscarinic antagonist used to cause bronchodilation and to decrease secretions for COPD/Asthma

Tiotropium (Spiriva)

55

Alpha Agonist used topically, has a longer duration than phenylephrine

Oxymetazoline (Afrin, Duration)

56

Nasal Spray containing phenylephrine

Neo Synephrine

57

Ephedrine isomer; Safe and effective... but can be utilized to make meth

Pseudoephedrine (Sudaphed)

58

Anti-Anginal drug that inhibits inward Na+ currents during cardiac action potentials to decrease intracellular calcium levels

Ranolazine (Ranexa)

59

Drug combinations to treat angina

- Hydralazine + Isosorbide Dinitrare (BiDil)
- Daily Beta Blockers + NG PRN

60

Cardiac or Digitalis Glycosides

Digoxin (Lanocxin)

61

Antianginal organic nitrate prototype that acts to dilate SYSTEMIC veins and arteries (major) and to improve coronary blood supply to ischemic areas (minor)

Nitroglycerin

62

Nonselective calcium channel blockers that have direct cardiac and vascular actions

Diltiazem (Cardizem) and Verapamil (Calan, Isoptin)