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Receptors > Pharm > Flashcards

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
Q

Uses of Epinephrine

A

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
Q

Toxicities of Epinephrine

A

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
Q

Ephedrine

A

similar to low dose Epinephrine… also inc NE release
high bioavailability long duration - effect may last hours
***CNS stimulant, cause broncodilation

28
Q

Dopamine (Intropin)

A

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
Q

Fenoldopham (Corlopam)

A

selective D1 rec agonist

** dilation of vascular beds, dec BP

30
Q

Amphetamine

A

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
Q

Cocaine

A

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
Q

Tyramine

A

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
Q

Phentolamine (Regitine)

A

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
Q

Phenoxybenzamine (Dibenzyline)

A

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
Q

Prazosin (Minipress)

A

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
Q

Uses of Prazosin

A

hypertension, benign prostatic hyperplasia

No inc in blood glucose

37
Q

Side effects of Prazosin

A

First dosage phenomenon (postural hypotension and syncope)
dizziness is common
nasal stuffiness

38
Q

Terazosin (Hytrin), Doxazosin (Cardura)

A 
similar to prazosin, a1 block
dec size of prostate
Tera- long half life (20 hours)
Doxa - longest half life
FDPhenom
39
Q

Tamsulosin (Flomax)

A

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
Q

Yohimbine

A

Alpha-2 selective antagonist - blocks presynaptic alpha 2 receptors –> INC NE
opposite of Clodine (BP and HR inc)
* dangerous for men with Hypertension

41
Q

Prototype drug for Beta-receptor Antagonist?

A

Propranolol (Inderal)

Beta receptor antagonists are widely used in may CVD

42
Q

Propranolol (Inderal)

A

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
Q

Pharmacokinetics of Propranolol

A

given orally, slowly absorbed, sustained release once a day preparation available.
Low bioavailability with extensive first pass metabolism.
GETS INTO BRAIN EASY.

44
Q

Uses of Propranolol

A

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
Q

Side Effects of Propanolol

A

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
Q

Drug interactions with Propanolol

A

Drugs that inhibit - cimetidine and chlorpromazine

Drugs that inc metabolism - barbituates, phenytoin, rifampin. SMOKING.

47
Q

Timolol (Timoptic)

A

non specific beta antagonist
eye treatment - glaucoma
absorbed systemically… should not be used with people with asthma

48
Q

Nadolol (Corgard)

A

doesnt get into the brain, less likely to cause sedation

no local anesthetic activity

49
Q

Sotalol (Betapace)

A

no local anesthetic activity

blocks calcium channels

50
Q

Metoprolol (Lopressor);Atenolol (Tenormin); Bisoprolol (Zebeta)

A

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
Q

Nebivolol (Bystolic)

A

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
Q

Esmolol (brevibloc)

A

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
Q

Beta-antagonists with ISA

A

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
Q

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.

A

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
Q

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.

A

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
Q

Clinical uses of B-blockers

A

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
Q

Reserpine

A

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
Q

Metyrosine (Demser)

A

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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