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Pharm Flashcards

1
Q

Beta-1 - Dobutamine

A

Inc HR/ inc AV conduction, velocity, and automaticity/ Inc renin secretion from kidney

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2
Q

Beta-2 - Albuterol

A

RELAX bronchioles, blood vessels supplying skeletal muscle/ promote K+ uptake into skeletal muscle/ inc glycogenolysis –> For ASTHMA

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3
Q

Beta-3 - No Agonist

A

inc lipolysis in fat cells

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4
Q

Dopamine-1

A

Dilation of renal blood vessels

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5
Q

Alpha-1 - Phenylephrine

A

Vasoconstriction in smaller blood vessels in the skin (inc peripheral vascular resistance)/ vasoconstrict in nasal mucosa (dec NASAL CONGESTION), mydriasis/ contract prostate

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6
Q

Alpha-2 - Clonidine

A

presynaptic nerve terminals/ inhibit transmitter release

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7
Q

NE effect on B2 receptors?

A

Little or none

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8
Q

Largest effect of alpha receptor stimulation?

A

On small BVs/ increases arterial resistance in BVs —> splanchic BVs have mainly alpha receptors. NET EFFECT = Inc Blood Pressure.

Inc BP will stimulate baroreceptors –> inc vagal input –> slow heart

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9
Q

Effect of alpha receptor on eye

A

activate radial pupillary dilator muscle –> mydriasis/ inc removal of aqueous humor, dec intraocular pressure

USED in GLAUCOMA (alpha agonist)

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10
Q

Alpha-1 - In respiratory tract

A

BVs in the upper airway and mucous membranes contain ALPHA-1 receptors… vasoconstrict by decongestants

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11
Q

Effect of Beta agonist on eye

A

inc production of aqueous humor –> inc intraocular pressure

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12
Q

Beta-2 - Genitourinary

A

relax uterus –> useful for premature contractions in pregnancy

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13
Q

Phenylephrine (Mydrin, Neofrin)

A

Alpha-1 agonist
vasoconstrict –> inc peripheral vascular resistance
diastolic goes up, so systolic accompanies it
inc blood pressure –> reflex dec in HR
DECONGESTANT (VasoC in nasal mucosa)
produces mydriasis… topical for eye exam to dilate

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14
Q

Pseudoephedrine (Sudafed)

A

similar to phenylephrine
OTC decongestant
caution with patients with hypertension

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15
Q

Tetrahydrozoline (Visine), Naphazoline (Naphcon, Clear Eyes), Oxymetazoline (Afrin)

A

DIRECT alpha agonist
Vasoconstriction - nasal mucosa and eye
Oxy - nasal spray ** also acts on alpha 2 receptors and can cause hypotension

ALL contraindicated in NA-glaucoma and hypertension

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16
Q

Clonidine (Catapres)

A

selective Alpha-2 agonist = CNS
Presynaptic terminals in the CNS DECREASE NE release
–> reduce sympathetic output to the periphery = dec BP
Orally or transdermal patch
** widely used treatment for hypertension

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17
Q

Apraclonidine (Iopidine) and Brimonidine (Alphagan)

A

used in eye to dec intraocular pressure by reducing AH through alpha-2 receptor mediated vasoconstriction

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18
Q

Tizanidine (Zanaflex)

A

alpha 2 agonist with less effect on BP than clonidine.

–> reduce muscle spasticity

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19
Q

Isoproterenol (Isuprel)

A

Very potent selective B1 and B2 agonist
inc rate and force of contraction of the heart
vasodilation in skeletal muscle
**dilation of skeletal BVs –> lead to decrease in BP (dec in BP leads to a reflex inc in HR)
EMERGENCY TREATMENT FOR CARDIAC ARREST AND COMPLETE HEART BLOCK
*large doses may cause tachycardia, palpitations and arrhythmias

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20
Q

Dobutamine (Dobutrex)

A

Beta-1 - selective agonist
(+) ionotropic effect in the heart
frequently used in cardiac stress

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21
Q

Albuterol (Ventolin)

A

Beta-2 - little effect on B1 in normal doses
ASTHMA
common side effects: tachycardia and skeletal muscle tremor

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22
Q

Norepinepherine (Levophed)

A

stimulates alpha and B1 (little effect on B2)
MUST BE INJECTED –> very short duration of action b/c high metabolism
effect primarily on BP
VC mediated by alpha Rs –> inc vascular peripheral resistance
as mean pressure in, baroreceptor reflex compensate for inc blood pressure and dec HR
** if Atropine given prior to NE –> vagal reflex inhibited (baroreceptor effect will not occur and HR will inc with no reflex)
CAN CAUSE SEVERE VC AT THE INFUSION SITE AND CAN CAUSE NECROSIS

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23
Q

Epinephrine (Adrenalin)

A

stimulates alpha, B1, and B2

MUST BE INJECTED SC OR IV… short duration of action

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24
Q

Explain Epinephrine effect

A
  1. Beta-1 inc HR and force of contraction
  2. Alpha-1 causes vasoconstriction in skin, mucosa, and kidney –> inc systolic and diastolic BP
  3. Beta-2 decreases diastolic BP b/c of dilation of BVs to skeletal muscle
  • -> pulse pressure changes, but not mean pressure so HR inc due to Beta stimulation
    • inc blood glucose
    • renin secretion increawes
    • FFAs concentration inc due to lipolysis in fat cells (B2)
25
Uses of Epinephrine
Anaphylactic shock Emergency treatment for cardiac arrest and complete heart block VC property used to dec diffusion of injected drugs such as local anesthetics B2 - Bronchodilation
26
Toxicities of Epinephrine
tremor, throbbing headache, inc BP, and tachycardia angina in patient with CAD ** one of the most potent vasopressors available, especially at high doses @ low doses, vasodilation dominates @ high doses, vasoconstriction occurs INJECTION OF EPI IS CONTRAINDICATED IN PEOPLE TAKING BETA-BLOCKERS... MAY LEAD TO SEVERE HYPERTENSION
27
Ephedrine
similar to low dose Epinephrine... also inc NE release high bioavailability long duration - effect may last hours ***CNS stimulant, cause broncodilation
28
Dopamine (Intropin)
low doses activate D1 receptors = vasodilation * inc renal blood flow, inc glomerular filtration and sodium excretion at HIGH concentration = simulates B1 --> (+) ionotropic and chronotropic effect ** given intravenously to treat CARDIAC SHOCK... INC cardiac output without causing VC --> Higher dose may also cause release of NE and stimulate alpha 1 = VC and inc BP
29
Fenoldopham (Corlopam)
selective D1 rec agonist | ** dilation of vascular beds, dec BP
30
Amphetamine
indirect-acting sympathomimetic ** inc release of NE from neurons, especially in the CNS - stimulant psychosis, increase alertness, dec diet, dec need for sleep, EUPHORIA --> Meth = more central actions and fewer peripheral effects --> methyphenidate (Ritalin) = children with attention deficit hyperactivity disorder
31
Cocaine
INHIBITS re-uptake of DA and NE into nerve terminals shorter acting and more intense than amphetamine ADDICTING may cause severe hypertension and stroke arrhythmias, MI, psychosis local anesthesia
32
Tyramine
inc release of catecholamines from nerve terminals, displaces NE --> forming false transmitter, octopamine NORMALLY hydrolyzed by monoamine oxidase (MAO) dont use with depressed patients
33
Phentolamine (Regitine)
Competitive agonist for both alpha receptors Dec peripheral resistance due to blockade of alpha-1 receptors alpha-2 receptors: baroreceptor reflex as well as increased NE release in the heart --> cardiac stimulation Hypotension is major toxicity ** may be used short-term treatment of hypertensive crisis
34
Phenoxybenzamine (Dibenzyline)
IRREVERSIBLE alpha blocker - binds covalently Inhibits reuptake of NE into presynaptic terminals (since there is some block of alpha 2 receptors, concentration of NE in the SC may increase) Tachycardia may occur from b1 stimulation and inc sympathetic stimulation due to lowered blood pressure ** Major theraputic use is treatment of pheochromocytoma Nasal stuffiness occurs due to decreased VC in the nasal mucosa
35
Prazosin (Minipress)
highly selective for ALPHA-1; less likely to cause relfex tachycardia relaxes both arterial and venous smooth muscle through A1 blockade --> decreases peripheral vascular resistance (BP drops) DECREASES PRELOAD TO HEART SO CO IS NOT LIKELY TO INC lack of A2 blockade reduces likelihood of reflex tachycardia duration = 7-10 hours (twice daily)
36
Uses of Prazosin
hypertension, benign prostatic hyperplasia | No inc in blood glucose
37
Side effects of Prazosin
First dosage phenomenon (postural hypotension and syncope) dizziness is common nasal stuffiness
38
Terazosin (Hytrin), Doxazosin (Cardura)
``` similar to prazosin, a1 block dec size of prostate Tera- long half life (20 hours) Doxa - longest half life FDPhenom ```
39
Tamsulosin (Flomax)
more selective for alpha-1A than alpha-1B alpha1A receptor subtype is prominent in prostate; alpha1B is most important in blood vessels Little effect on BP ** relaxes prostate, base of bladder, and bladder sphincter -->easier urination ****TREAT BPH - main SE is difficulty of ejaculation afluzosin is similar drugs for BPH. Dizziness.
40
Yohimbine
Alpha-2 selective antagonist - blocks presynaptic alpha 2 receptors --> INC NE opposite of Clodine (BP and HR inc) * dangerous for men with Hypertension
41
Prototype drug for Beta-receptor Antagonist?
Propranolol (Inderal) | Beta receptor antagonists are widely used in may CVD
42
Propranolol (Inderal)
non-selective competitive antagonist w/ equal affinity for both B1 and B2 ** Slows heart rate and dec force of contraction Dec RENIN release Dec lipolysis and glycogenolysis ** Local anesthetic-like blockade of Na+ channels at higher doses
43
Pharmacokinetics of Propranolol
given orally, slowly absorbed, sustained release once a day preparation available. Low bioavailability with extensive first pass metabolism. GETS INTO BRAIN EASY.
44
Uses of Propranolol
CHRONIC use decreases blood pressure - widely used treatment for hypertension. Dec mortality rate in people with MI Used to treat Angina and Arrhythmias Useful to slow heart and decrease BP in hyperthyroidism PREVENT MIGRAINE reduces portal vein pressure and may decrease risk of bleeding in patients with cirrhosis Dec tremor and stage fright
45
Side Effects of Propanolol
Bronchoconstriction in asthmatics! Depression of myocardial contractility and excitability may induce or exacerbate heart failure in late stages of congestive heart failure Slowing of AV conduction may cause bradycardia **Should not be discontinued abruptly --> cardiac arrhythmias. Sedation, fatigue and possibly depression occur due to CNS penetration mask symptoms of hyperthyroidism and hypoglycemia
46
Drug interactions with Propanolol
Drugs that inhibit - cimetidine and chlorpromazine | Drugs that inc metabolism - barbituates, phenytoin, rifampin. SMOKING.
47
Timolol (Timoptic)
non specific beta antagonist eye treatment - glaucoma absorbed systemically... should not be used with people with asthma
48
Nadolol (Corgard)
doesnt get into the brain, less likely to cause sedation | no local anesthetic activity
49
Sotalol (Betapace)
no local anesthetic activity | blocks calcium channels
50
Metoprolol (Lopressor);Atenolol (Tenormin); Bisoprolol (Zebeta)
selective B1 blockade effects predominately on heart Widely used to treat hypertension used for migraine prophylaxis Provide better exercise tolerance because they do not block dilation of B2 receptors Less likely to inhibit glycogenolysis *** Atenolol has recently been shown to increase risk of Type II diabetes Use with caution with patients who have COPD If high doses are used, B2 receptors can be effects --> Betaxolol (Betopic) is a selective B1 blocker used for treatment in glaucoma.
51
Nebivolol (Bystolic)
Beta blocker that also produces vasodilation due to release of NO from endothelial cells MOST SELECTIVE for B1 receptors better effect on Bp and have fewer side effects Causes significant reductions in cholesterol, TGs, and blood glucose
52
Esmolol (brevibloc)
B1 selective antagonist with very short duration of action hydrolyzed by esterases in RBCs 1/2 life = 8 min MUST be injected intravenously *Use when very short B Blockade is wanted, when rapid effect is needed.
53
Beta-antagonists with ISA
PARTIAL AGONISTS - stimulate receptors with sympathetic activity is low and block them when it's high **Pindolol (Visken), Carteolol are all non-selective B blockers which have some intrinsic activity **Acebutolol (Sectral) is a selective B1 antagonist with intrinsic activity Treat hypertension and angina Risk of Bradycardia may be lower, since they will not decrease HR as much Also, may not affect plasma lipids as much as other non-selective beta blockers ** Carteolol (Ocupress) is used in the eye to treat glaucoma; may cause stimulation of B2 receptors
54
Labetalol (Normodyne) Norman is the chillest (relax arterial SM and dec BP) and didnt work hard (no tachycardia). Unfortunately he had a hypertensive emergency and the intravenous injection did not work.
Blocks B1 and B2, and A1 receptors A1 blockade - leads to relaxation of arterial smooth muscle and decreased blood pressure B1 block - prevents compensatory increase in heart rate, so that the dec in BP is less likely to cause tachycardia than when alpha-blockers are used alone Treatment of hypertension Intravenously in hypertensive emergencies
55
Carvedilol (Coreg) Coreg the Corgi is a bitch (non-selective B blocker), but was once the first Alpha dog (A1 blocker). Even though he was a bitch, he didn't stress about life. He had some dilated pupils and didn't like to play competitive BP because he wasnt Tacky (tachycardia). He liked to bite this radical dog mito. His owner had CHF, but helped improve his life.
Non-selective B blocker which also blocks A1 Vasodilation and decreases BP without causing Tachycardia dec free radicals and inhibits vascular smooth muscle mitogenesis Treatment for hypertension improves mortality and morbidity in treatment of CHF
56
Clinical uses of B-blockers
hypertension: now usually drugs of 3rd or 4th choice due to adverse effects Ischemic heart disease: improves survival following myocardial infarction; improves exercise tolerance in angina; and, in the early stages of congestive heart failure, prolongs lifespan Cardiac arrhythmias: ventricular and supraventricular arrhythmias are treated with B-blockers Obstructive cardiac myopathy: improves SV Dissecting aortic aneurysm: decreases development of systolic pressure and reduces the rate which force increases in the myocardium.
57
Reserpine
interferes with the uptake and storage of biogenic amines in nerve terminals Will cause depletion of NE, Dopamine, Serotonin from both the peripheral nerve terminals and the brain Low doses dec BP, side effects include severe diarrhea, depression, sedation, and parkinson's like symptoms
58
Metyrosine (Demser)
tyrosine analogue, blocks tyrosine hydroxylase * rate limiting step in the synthesis of dopamine - -> dec amount of NE and Epi that can be produced. Pre-surgical treatment of pheochromocytoma

Receptors (1 decks)

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