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35 Cards in this Set

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Does Prozasin have a high or low first pass effect?
High
What is the receptor affinity for this antagonist Phenoxybenzamine? Action? Tx? When does it decrease BP the most? it it revesible?
Phenoxybenzamine: (1) Affinity: IRREVERSIBLE ∂ antagonist: ∂1>∂2… (2) Action: (a) blocks reuptake of NE… (b) decreases BP when sympathetic tone is high…

(3) Tx: Pheochromocytoma, reduces BP in standing position
None
What are the 5 ADR of Phenoxybenzamine?
postural hypotension, tachycardia, nasal stuffiness, inhibits ejaculation, CNS effects (enters brain)
Name the 3-∂ antagonist and the one -∂-agonist?

Which one of these enters the CNS?

Which one is a prodrug?
Phentolamine, Prozasin, Phenoxybenzamine, Midodrine

2) Phenoxybenzamine enters the CNS

3) Midodrine is a prodrug
None
Name the 5 ß-blocking drugs.
Proproanolol, pindolol, meoprolol, atenolol and labetalol
None
Name the one combination ß1/ß2/∂1 blocking drug.
Carvedilol
None
Which of the alpha antagonists is irreversible?
Phenoxybenzamine
What is the receptor affinity for this AGONIST Midodrine? Action? Tx?

Is there CNS activity?
Midodrine… This is an AGONIST:

(1) Affinity: Selective ∂1 AGONIST Selective ∂1…

(2) Action: Prodrug… No ß adrenergic activity, No NE release stimulation, no CNS activity…

(3) Tx: hypotensin

(4) No CNS activity
None
Out of these drugs which is the prodrug, and (2) which would potentiate antidepressant durgs?: Phentolamine, Prozasin, Phenoxybenzamine, Midodrine, Proproanolol, pindolol, meoprolol, atenolol, labetalol, carvedilol
(1) Prodrug: Midodrine… (2) Potentiate antidepressants: Pindolol
What are Midodrine's ADR and contraindications?
Midorines ADR: Supine hypertension if given at night… (1) Contraindicated: diabetes because ∂ agonists increase glucogenesis
None
What is the receptor affinity for this antagonist Phentolamine? Action? Tx? Diagnostic use? ADR?

Which of the ∂ antagonists is IRREVERSIBLE?
Phentolamine:
(1) Affinity: Pure Competitive ∂ antagonist ∂1=∂2:

(2) Action: (a) decrease peripheral resistance (w/o ∂1)… (b) increase NE release (w/o ∂2)…

(3) Tx:
(a) pheochromocytoma (excessive release of catacholamines due to adrenal tumor)

(b) erectile dysfunction.

(4) diagnosis of pheochromocytoma (patients w/ tumor have a greater drop in pressure than those w/ primary HTN.

(5) May cause baroreceptor mediated tachycardia... nasal congestion

(6) Phenoxybenzamine
None
Which of the alpha antagonists is used for BPH?
Prozasin
What is the receptor affinity for this antagonist Propranolol? Action? Tx?
Propranolol: (1) Affinity: Pure competitive ß antagonist… (2) Action: ß antagonist… (3) Tx: HTN, anginia, V-arrythmia, MI, pheochromocytoma, migraine prophylaxis…
What are the 3 ADR of Phentolamine?
reflex tachycardia, nasal congestion, orthostatic hypotension
Out of these drugs which are (1) partial agonists and (2) which has a low bioavailability: Phentolamine, Prozasin, Phenoxybenzamine, Midodrine, Proproanolol, pindolol, metoprolol, atenolol labetalol, carvedilol…
(1) Partial agonists: pindolol, Labetalol… (2) low bioavailability: Propranolol
None
What are the ADRs of Propranolol? What are the contraindications?
Propranolol: ADRs: bradycardia, neg inotrope, decreased CO, bronchoconstriction, exercise intolerance, fatigue, sleep disturbance… (2) counterindications: diabetes melitus due to ß response to hypoglycemia is stunted
Which of the alpha drugs is a prodrug?

Which alpha drug enters the CNS/brain?
Midodrine is a prodrug

Phenoxybenzamine enters the CNS
None
What is the receptor affinity for this antagonist Prazosin? Action? Tx?
Prazosin: (1) Affinity: highly selective competitive ∂1 antagonist… (2) Action: relaxes smooth muscle of vasculature and prostate… (3) Tx: HTN and BPH
Propranolol: what is its bioavailability? Where is it metabolized? Is its therapeutic index wide or narrow?
Propranolol: Bioavailability: 26%… Metabolized in gut… Narrow therapeutic index
Of the ß blockers, which do not have membrane stabilizing activity?
Atenolol and Metoprolol
Which of the alpha drugs blocks reuptake of NE?
phenoxybenzamine
Which 2 of the alpha antagonists are used for Pheochromocytoma?
Phentolamine, phenoxybenzamine
What is the receptor affinity for this antagonist Pindolol? Action? Tx? ADR?
Pindolol:
(1) Affinity:- Pure competitive β-antagonist/PARTIAL AGONIST.

(2) Action:
Antagonist: in presence of intrinsic agonist
(b) PARTIAL AGONIST in absence of intrinsic agonist…
(3) Tx: HTN, angina.

(4) May potentiate antidepressant meds (D)
None
Which of the alpha antagonists are used HTN?
Prozasin and Phenoxybenzamine
What is the receptor affinity for this antagonist Metoprolol? Action?

What are 5 main uses for this drug????
Metoprolol: (1) Affinity: Pure β1-antagonist… (2) Action: (a) No ISA or membrane stabilizing activity… (b) Slightly lipophilic… (3) Tx: stable angina, CHF, HTN, migraines, MI
None
Which of the alpha antagonists is used for erectile dysfunction?
Phentolamine
What is Metoprolol contraindicated in?
Metoprolol Contraindication: acute MI tx, high order heart block tx… (debatable: β blockers preferred in those with diabetes or peripheral vascular disease)
None
What is the receptor affinity for this antagonist Atenolol? Action? Tx?
Atenolol: (1) Affinity: Competitive β1 antagoinist… (2) Action: No ISA or MSA… (3) Tx: HTN
None
Which of the alpha antagonists can be used to diagnose pheochomocytoma?
Phentolamine
Which of the alpha antagonists will cause a decrease in BP when sympathetic tone is highest?
Phenoxybenzamine
What are the contraindications for Atenolol?
Atenolol Contraindicated: Better beta blocker for diabetes or peripheral vascular disease patients (β2 blocker bad)
Which drugs are contraindicated for Diabetes? Why?
Midodrine (Contraindicated: diabetes because ∂ agonists increase glucogenesis)… ß-blocking drugs (counterindications: diabetes melitus due to ß3 response to hypoglycemia is stunted)… At
What is the receptor affinity for this antagonist Labetalol? Action? Tx?
Labetalol: (1) Affinity:
(a) Competitive β antagonist/parial agonist@ ß receptors

(b) α1 antagonist…

(2) Action: racimic mixture… ISA at β receptors… (3) Tx: HTN
None
What is the ADR of Labetalol?
Labetalol ADR: hepatic failure
What is the receptor affinity for this antagonist Carvedilol? Action? Tx?
"Carvedilol: (1) Affinity: Blocks β1, β2, α1…

(2) Action: has antioxidant, antiproliferative effects, No ISA, Can vasodilate...

(3) Tx: CHF
None