[ANS] Antagonists/Sympatholytics - Alpha and Beta blockers

● Phenoxybenzamine

● Phentolamine

Nonselective alpha blockers include:

Nonselective alpha blockers

The following drugs are classified as:

● Phenoxybenzamine

● Phentolamine

● inhibits ALPHA receptor (pheochromocytoma)

● inhibits HISTAMINIC receptor (mastocytosis)

● inhibits 5-HT receptor (carcinoid syndrome)

[NONSELECTIVE ALPHA BLOCKERS]

MOA of phenoxybenzamine:

Phenoxybenzamine

[NONSELECTIVE ALPHA BLOCKERS]

This alpha blocker is IRREVERSIBLE and NONCOMPETITIVE.

Phenoxybenzamine

[NONSELECTIVE ALPHA BLOCKERS]

This alpha receptor antagonist is used in PHEOCHROMOCYTOMA (tumor in adrenal medulla) as PRESURGICAL TREATMENT and management of HYPERTENSIVE CRISIS in inoperable tumor.

Pheochromocytoma as:

● Presurgical treatment

● Management of hypertensive crisis in inoperable tumor

[NONSELECTIVE ALPHA BLOCKERS]

Phenoxybenzamine (as alpha blocker) is used in:

Phenoxybenzamine

[NONSELECTIVE ALPHA BLOCKERS]

This HISTAMINIC receptor antagonist is used in MASTOCYTOSIS.

Mastocytosis

[NONSELECTIVE ALPHA BLOCKERS]

Phenoxybenzamine (as histaminic blocker) is used in:

Phenoxybenzamine

[NONSELECTIVE ALPHA BLOCKERS]

This 5-HT receptor antagonist is used in CARCINOID SYNDROME (tumor found in enterochromaffin cell), which provides SYMPTOMATIC RELEASE.

Carcinoid tumor to provide symptomatic release

[NONSELECTIVE ALPHA BLOCKERS]

Phenoxybenzamine (as 5-HT blocker) is used in:

Phentolamine

[NONSELECTIVE ALPHA BLOCKERS]

This alpha blocker is REVERSIBLE and COMPETITIVE.

● Sympathomimetic poisoning

● Management of pheochromocytoma

● Raynaud syndrome (digital necrotic due to extreme climate)

● Erectile dysfunction

[NONSELECTIVE ALPHA BLOCKERS]

Phentolamine is used in the treatment of :

Phentolamine

[NONSELECTIVE ALPHA BLOCKERS]

This nonselective alpha blocker is used in the treatment of SYMPATHOMIMETIC POISONING.

Phentolamine

[NONSELECTIVE ALPHA BLOCKERS]

This nonselective alpha blocker is used in the MANAGEMENT of PHEOCHROMOCYTOMA.

Phentolamine

[NONSELECTIVE ALPHA BLOCKERS]

This nonselective alpha blocker is used in the treatment of RAYNAUD SYNDROME (digital necrotic due to extreme climate).

Phentolamine

[NONSELECTIVE ALPHA BLOCKERS]

This nonselective alpha blocker is used in the treatment of ERECTILE DYSFUNCTION, which is SAFER as it is locally injected.

● Vasodilators:

- Prazosins

- Doxazosins

- Terazosins

● Benign Prostatic Hyperplasia (BPH):

- Tamsulosin

- Alfuzosin

- Silodosin

● HORMONES:

- Finasteride

- Dutasteride

Alpha-1 selective blockers include:

Alpha-1 blockers (vasodilators in HTN)

The following drugs are classified as:

● Prazosins

● Doxazosins

● Terazosins

● Prazosins

● Doxazosins

● Terazosins

[ALPHA-1 BLOCKERS]

These alpha-1 blockers are used as VASODILATORS (ANTIHYPERTENSIVES):

1st dose phenomenon (Orthostatic hypotension, syncope)

[ALPHA-1 BLOCKERS]

Alpha-1 blockers cause __________, so the drugs must be taken at BEDTIME.

● Tamsulosin

● Alfuzosin

● Silodosin

[ALPHA-1 BLOCKERS]

These alpha-1 blockers are used in BPH for SYMPTOMATIC relief of urine retention.

Alpha-1 blockers (BPH)

The following drugs are classified as:

● Tamsulosin

● Alfuzosin

● Silodosin

● Finasteride

● Dutasteride

[ALPHA-1 BLOCKERS]

These HORMONES are used in BPH if there is a PROSTATE ENLARGEMENT.

Hormones (BPH)

The following drugs are classified as:

● Finasteride

● Dutasteride

● Yohimbine

● Rauwolscine

[ALPHA-2 BLOCKERS]

Alpha-2 blockers include:

Alpha-2 blockers

The following drugs are classified as:

● Yohimbine

● Rauwolscine

● Inotropy

● Chronotropy

● Dromotropy

[BETA BLOCKERS]

Beta-1 antagonism mostly occurs in the heart, decreasing _______ and resulting in cardiac depression.

● based on SELECTIVITY

● based on ADDITIONAL MOA

[BETA BLOCKERS]

Classes of beta blockers:

Bronchoconstriction

[BETA BLOCKERS - SELECTIVITY]

Selective beta-2 blockers cause _________, which are contraindicated in patients with BRONCHIAL ASTHMA and COPD.

● Nadolol

● Sotalol

● Timolol

● Propranolol

● Carteolol

● Carvedilol

● Labetalol

● Penbutolol

● Pindolol

[BETA BLOCKERS - SELECTIVITY]

Selective beta-2 blockers include:

Sotalol

[BETA BLOCKERS - SELECTIVITY]

This beta-2 blocker is the only class III beta blocker ANTI-ARRHYTHMIC.

Timolol

[BETA BLOCKERS - SELECTIVITY]

This beta-2 blocker is used as an ANTI-GLAUCOMA.

Propranolol (Inderal)

[BETA BLOCKERS - SELECTIVITY]

This is the PROTOTYPE beta-blocker (brand name: INDERAL)

● Celiprolol

● Bisoprolol

● Betaxolol

● Esmolol

● Acebutolol

● Atenolol

● Metroprolol

● Nebivolol

[BETA BLOCKERS - SELECTIVITY]

Beta-1 selective beta blockers include:

● Intrinsic Sympathomimetic Activity (ISA)

● Membrane stabilizers

● Vasodilation

[BETA BLOCKERS - ADDITIONAL MOA]

Additional moa of beta blockers include:

Beta-2 AGONIST

● Carteolol

● Celiprolol

● Labetalol

● Acebutolol

● Pindolol

● Penbutolol

[BETA BLOCKERS - ADDITIONAL MOA]

These beta blockers have Intrinsic Sympathomimetic Activity (ISA).

● Propranolol

● Acebutolol

● Labetalol

● Metoprolol

[BETA BLOCKERS - ADDITIONAL MOA]

These beta blockers are MEMBRANE STABILIZERS which are used as LOCAL ANESTHESIA.

Eyes (CORNEAL INJURY)

[BETA BLOCKERS - ADDITIONAL MOA]

Beta blockers that are MEMBRANE STABILIZERS display risk in the _______.

● Propranolol

● Acebutolol

● Labetalol

● Metoprolol

● Alpha-1 blockade

● Enhancing nitric oxide level

[BETA BLOCKERS - ADDITIONAL MOA]

Beta blockers can cause VASODILATION through:

● Carvedilol

● Labetalol

[BETA BLOCKERS - ADDITIONAL MOA]

Beta blockers that can cause VASODILATION through ALPHA-1 BLOCKADE include:

Nebivolol

[BETA BLOCKERS - ADDITIONAL MOA]

Beta blockers that can cause VASODILATION through enhancing NITRIC OXIDE level include:

Nebivolol

[BETA BLOCKERS - ADDITIONAL MOA]

This is the MOST CARDIOSELECTIVE BETA BLOCKER.

● Cardiovascular disorders

● Eye disorders

● Endocrine disorders

● Migraine/Stage fright

[BETA BLOCKERS - USES]

Beta blockers are used in:

● First line agent for hypertension in patient with history of post myocardial infarction

● Management of angina pectoris

● Management of stable heart failure

● Management of arrhythmia

[BETA BLOCKERS - USES]

Beta blockers are used in cardiovascular disorders as:

post myocardial infarction

[BETA BLOCKERS - USES]

Beta blockers are used as first line agent for hypertension in patient with history of _________.

● Bisoprolol

● Carvedilol

● Metoprolol SUCCINATE

● Nebivolol

[BETA BLOCKERS - USES]

Beta blockers used in STABLE heart failure include:

Sotalol

[BETA BLOCKERS - USES]

Beta blockers are used in ARRHYTHMIAS (class II) except ________ which is under class III.

● Timolol

● Betaxolol

[BETA BLOCKERS - USES]

Beta blockers used in GLAUCOMA.

● Propranolol (SEDATING)

● Carvedilol (NON-SEDATING)

[BETA BLOCKERS - USES]

Beta blockers used in the treatment of sympathetic symptom of HYPERTHYROIDISM such as TACHYCARDIA as they inhibit peripheral conversion of T4 to T3.

Propranolol

[BETA BLOCKERS - USES]

This beta blocker is used as PROPHYLAXIS in MIGRAINE HEADACHE.

Propranolol

[BETA BLOCKERS - USES]

This beta blocker is used in the treatment of STAGE FRIGHT.

● Bradycardia ( heart rate < 60 bpm)

● Mask hypoglycemic symptom which is tachycardia

● Bronchoconstriction

● Hyperlipidemia

[BETA BLOCKERS - TOXIC EFFECTS]

Toxic effects of beta blockers include:

Tachycardia

[BETA BLOCKERS - TOXIC EFFECTS]

Beta blockers mask the symptom of HYPOGLYCEMIA which is _______.

Beta-2 blockers

[BETA BLOCKERS - TOXIC EFFECTS]

Beta blockers that can cause BRONCHOCONSTRICTION:

Beta-3 blockers (lipolysis)

[BETA BLOCKERS - TOXIC EFFECTS]

Beta blockers that can cause HYPERLIPIDEMIA: