MA.

CARLA
C. CACHUELA
BSN2A
ALPHA-SPECIFIC
ADRENERGIC
AGONISTS

Ready!
 Learning
Overview on Alpha-specific
Adrenergic Agonists 01
Objectives:
Therapeutic Actions
of Alpha-Agonists 02
Indications of
Alpha-Agonists 03
Pharmacokinetics
of Alpha-Agonists 04
 Learning
Contraindications of
Alpha-Agonists 05
Objectives:
Adverse Effects of
Alpha-Agonists 06
Drug-drug Interactions
of Alpha-Agonists 07
General Pharmacology
of Alpha-Agonists 08
What are Alpha-specific
Adrenergic Agonists
Also called as alpha-agonists, which are drugs that
bind primarily to alpha-receptors rather than to
beta-receptors.
What are Alpha-specific
Adrenergic Agonists
These alpha-receptors are located on the arteries of
the heart.
What are Alpha-specific
Adrenergic Agonists
Three drugs belong to this class:
1. Clonidine
(Catapres)

2. Midodrine
(ProAmatine)

3. Phenylephrine
(Neo Synephrine, Allerest,
AK-Dilate, etc.)
Clonidine
(Catapres)

Clonidine is a medication
used to treat high blood
pressure and certain
pain conditions.

It is used by mouth, by
injection, or as a skin
patch.
Midodrine
(ProAmatine)

Midodrine is used
to treat orthostatic
hypotension.

It works by causing
blood vessels to tighten,
Which increases blood
pressure.
Phenylephrine
(Neo-Synephrine, Allerest, AK-Dilate, etc.)

Phenylephrine is used
to relieve nasal discomfort
caused by colds, allergies,
and hay fever.

It is also used to relieve

Sinus congestion and
pressure.
Therapeutic Actions
and Indications
• Therapeutic effects of the
alpha-agonists results
from the stimulation of
alpha receptors within the
SNS.

• The uses are varied,

depending on the specific
drug and the route of
administration.
Therapeutic Actions
and Indications
1. Phenylephrine- is used in many
combination cold and allergy products.

Parenterally:
• treat shock or shock-like states
• paroxysmal supraventricular tachycardia
• prolong local anesthesia
• maintain blood pressure
Therapeutic Actions
and Indications
1. Phenylephrine- is used in many
combination cold and allergy products.

Topically:
it is used to treat allergic
rhinitis and to relieve the symptoms of
otitis media.
Therapeutic Actions
and Indications
1. Phenylephrine- is used in many
combination cold and allergy products.
Ophthalmically:
• dilate the pupils for eye examination
• before surgery
• elevated eye pressure for glaucoma
Therapeutic Actions
and Indications
Orally:
Midodrine is an oral drug that is used to
treat orthostatic hypotension in patients
who do not respond to traditional therapy.
 Therapeutic Actions
and Indications
Orally:
Clonidine is available in oral form to control
hypertension.

Transdermally:
Clonidine is available in injection for
epidural infusion to control pain in
cancer patients
Pharmacokinetics
These drugs are generally well absorbed
from all routes of administration and
reach peak levels in a short period
of 20 to 45 minutes.

They are widely distributed in

the body, metabolized in the
liver, and primarily excreted
in the urine.
 Pharmacokinetics
Phenylephrine- is used in many
combination cold and allergy
products.
Phenylephrine can be given intramuscularly,
subcutaneously, IV, orally, and as a nasal or
an ophthalmic solution.
 Contraindications and Cautions

The alpha-specific adrenergic They should be used with caution

agonists are contraindicated in in the presence of CV disease or
the presence of allergy to the Vasomotor spasm.
specific drug.

There are no adequate They should be used

studies about use during with caution in the
pregnancy and lactation. presence renal or
hepatic impairment.
 Adverse Effects—CNS

Blurred vision and

sensitivity to light. Feelings of anxiety,
restlessness, depression,
Strange dreams and and fatigue.
personality changes.
 Adverse Effects—CV

Effects can include

arrhythmias, ECG changes,
blood pressure changes, and
peripheral vascular problems.
 Adverse Effects—GI and SNS

Nausea, vomiting,
and anorexia can occur,
related to the depressant
effects of the SNS on the GI tract.
 Adverse Effects— Genitourinary

Effects can include changes in

sexual function related to the Effects can include decreased
Sympathetic stimulation urinary output, difficulty
of these systems. urinating, and dysuria.
Clinically Important Drug–Drug Interactions
Any adrenergic agonist will lose effectiveness if combined
with any adrenergic antagonist.
Clinically Important Drug–Drug Interactions

Phenylephrine combined with MAOIs

Which can cause severe hypertension,
headache, and hyperpyrexia
Clinically Important Drug–Drug Interactions

Increased sympathomimetic effects occur

when Phenylephrine is combined with TCAs.
Clinically Important Drug–Drug Interactions

Midodrine can precipitate

increased drug effects of
digoxin, beta-blockers, and
many antipsychotics.
Clinically Important Drug–Drug Interactions

Clonidine has a decreased

antihypertensive effect if
taken with TCAs.

Clonidine causes paradoxical

hypertension if combined
with propranolol.
General Pharmacology
Most α-agonists that are used
therapeutically are relatively
selective for either α1 or α2-adrenoceptors.
α1-adrenoceptor agonists
(systemic vasoconstrictors)

α2-adrenoceptor agonists
(centrally-acting vasodilators)
 α1-adrenoceptor agonists
(systemic vasoconstrictors)

● Medications causing vasoconstriction, usually results in an increase

in systemic blood pressure, but it may also occur in specific tissues,
causing a localized reduction in blood flow.

Medications:
● Methoxamine

● Phenylephrine

● Oxymetazoline

● Tetrahydrozoline

● Xylometazoline
 α1-adrenoceptor agonists
(systemic vasoconstrictors)

● Medications causing vasoconstriction, usually results in an increase

in systemic blood pressure, but it may also occur in specific tissues,
causing a localized reduction in blood flow.

● Methoxamine
● Phenylephrine

HYPOTENSION SHOCK
 α1-adrenoceptor agonists
(systemic vasoconstrictors)

● Medications causing vasoconstriction, usually results in an increase

in systemic blood pressure, but it may also occur in specific tissues,
causing a localized reduction in blood flow.
● Oxymetazoline
● Tetrahydrozoline
● Xylometazoline
● Phenylephrine

NASAL DECONGESTANT
 α2-adrenoceptor agonists
(centrally-acting vasodilators)

● Are medications that opens or (dilate) blood vessels.

● As a result, blood flows more easily through your vessels.

Medications:
● Clonidine

● Guanabenz

● Guanfacine

● α -methyldopa

HYPERTENSION
ALPHA-SPECIFIC
ADRENERGIC
AGONISTS
Learning
Overview on Alpha-specific
Adrenergic Agonists 01
Check:
Therapeutic Actions
of Alpha-Agonists 02
Indications of
Alpha-Agonists 03
Pharmacokinetics
of Alpha-Agonists 04
Learning
Contraindications of
Alpha-Agonists 05
Check:
Adverse Effects of
Alpha-Agonists 06
Drug-drug Interactions
of Alpha-Agonists 07
General Pharmacology
of Alpha-Agonists 08
THANK
YOU FOR
WATCHING!
 REFERENCES:
● Hasdai, D., Berger, P., Battler, A., & Holmes, D. (Eds).
(2010). Cardiogenic shock. Totowa, NJ: Humana Press.
● Karch, A. M. (2011). 2012 Lippincott’s nursing drug guide.
Philadelphia, PA: Lippincott Williams & Wilkins.
● National Center for Complementary and Alternative
Medicine (2004). Consumer Advisory: Ephedra.
Available at: http://nccamnih.gov/hea lth/alerts
ephedra/consumeradvisory.htm.
● Porth, C. M. (2010). Pathophysiology: Concepts of altered
health states (8th ed.). Philadelphia, PA: Lippincott
Williams & Wilkins. 66485457-66485438