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24 Cards in this Set

  • Front
  • Back
Norepinephrine (Levophed)
A1, A2, B1 Agonist

Rarely uses as a drug in modern medicine.

Used IV, rapidly degraded orally

Toxicity: Cardiac Arrythmias, Hypertension, Anxiety, Palpitations, Headache, Decreased Flow to Kidneys
Epinephrine (Adrenalin)
A1, A2, B1, B2 Agonist

Uses:
1) Parenteral Injection as a cardiac stimulant in emergencies
2) Inhalation or injection as a bronchial dilator
3) The two above make it good for management of Anaphylactic Shock (Type 1 Hypersensitivity)!
4) Topically for Glaucoma
5) Hemostasis during Surgery: Vasoconstrictor Agent in many local anesthetic preparations (limits diffusion of anesthetic and increases duration of action)
Phenylephrine (Neo-Synephrine)
Selective A1 Agonist

Uses: Primarily as a Vasoconstrictor
1) Topically to Nasal Mucosa: Vasoconstriction shrinks nasal mucosa, allowing free flow of air. Also reduces mucus secretion.
2) Systemically to raise BP in Neurogenic Hypertension
3) Systemically to induce Vagally-Mediated Reflex Slowing of the Heart in Paroxysmal Tachycardia
4) Topically in eye to induce Mydriasis (without affecting accommodation)

Much longer duration of action relative to catechols
Clonidine (Catapres)
Selective A2 Agonist

Uses:
1) Antihypertensive Drug by Oral Administration
2) Withdrawal from Narcotic Addiction

CNS Effects Predominate!
Dobutamine (Dobutrex)
Somewhat selective B1 Agonist

Uses:
1) Stimulate the heart in cases of Cardiogenic Shock
Metaproterenol (Metaprel)
Relatively selective B2 Agonist

Should be used "as needed only" since chronic use wthout steroids can mask underlying inflammation!

Others include:
1) Formoterol
2) Albuterol
3) Salmeterol (Most Selective, Partial)
4) Terbutaline


Uses: Orally or Inhalation
1) Dilate Bronchial Airways in management of reversible airway diseases (Asthma, COPD)
Isoproterenol (Isuprel)
B1 and B2 Agonist

Uses:
1) Bronchial Dilator via Inhalation

Side Effects: Induces Tachycardia more frequently than selective B2 Agonists!
Ephedrine
A1, B1, B2 Agonist

Natural Plant Alkaloid

Acts mainly INDIRECTLY via release of NE and E, but ALSO Directly!

Unlike Catecholamines, it is NOT destroyed by GI Tract and Liver. Thus, given Orally.

Uses:
1) Relax Bronchial Muscle
2) Vasoconstriction of Vessels in the Nasal Mucosa
3) Elevate BP

Can penetrate into the brain and produce Amphetamine-like arousal and CNS Stimulation.
Dopamine (Intropin)
Uses as I.V. Drip in management of Hypotensive Shock

Uses:
1) Moderate to Low Doses: D1 Agonist actions produce Relaxation of Vascular Smooth Muscle in Renal Blood Vessels and Improves Renal Blood Flow
2) Higher Doses: Effects at Cardiac B1 to Increase Contractility
3) Still Higher Doses: Recruit actions at A1 to produce Vasoconstriction and Raise BP

Rapidly inactivated by Hepatic MAO
Tyramine
Prototype Indirectly Acting Adrenergic Amine (Promote release of Endogenous NE from its stores)
Amphetamines
Mixed Action Dug: Produce effects by direct receptor stimulation AND indirectly through release of NE

Absence of BOTH Ring Hydroxyls:
1) Increased Oral Effectiveness and Duration of Action
2) Penetrates BBB

Presence of an alpha-carbon substituent: enhanced resistance to MAO
LABAs
Long Acting B2AR Agonists:

The MOST Selective B2 Agonists

1) Salmeterol
2) Formoterol

Uses:
1) Prophylactic treatment of nocturnal as well as relatively mild but chronic asthma

Should NEVER be used alone, should only be used as an add-on following corticosteroid treatment!
Prazosin (Minipress)
Prototype Competitive A1 ANTagonist

Uses:
1) Management of Mild to Moderate Hypertension (Oral or IV)
2) Heart Failure (to reduce preload and after load)
3) Benign Prostatic Hypertrophy (BPH)

Side Effects:
1) Postural Hypotension
2) Inhibits Ejaculation 5-10%
Phentolamine
Non-Selective Reversible A ANTagonist

Dirty drug since it also inhibits responses to Serotonin and is an Agonist at Muscarinic and Histamine Receptors!
Phenoxybenzamine
Non-Selective Irreversible A ANTagonist - Covalent Bond

Uses:
1) Pheochromocytoma (Adrenal Tumor)
2) Erectile Dysfunction

Side Effects:
1) Postural Hypotension
2) Drug-Induce Tachycardia
Labetol
Non Selective Reversible A ANTagonist available as racemic mixture:

(S,R) --> Potent A1 Selective Antagonist

(R,R) --> Potent B Antagonist

Uses:
1) Treatment of Hypertension with less Tachycardia as a side effect
Yohimbine
Selective A2 ANTagonist

Natural Plant Alkaloid

Uses: None currently, but may be useful in future:
1) Depression
2) Painful Diabetic Neuropathies
3) Male Impotence secondary to Diabetes
Propranolol (Inderal)
Non-Selective B ANTagonist

Uses:
1) Hypertension
2) Cardiac Arrhythmias
3) Angina Pectoris
4) Migraine
5) Anxiety

Very lipophilic --> Crosses BBB. Golfers, shooters, and pool hall addicts love this drug because it reduces Tremor.

Side Effects:
1) Depresses Contractility and should be used with great care in patients with heart failure
2) Can exacerbate Asthma, COPD, Emphysema
3) HAZARDOUS to give to individuals receiving Hypoglycemic Drugs (Insulin Dep Diabetes) or who are prone to serious allergies
Timolol (Timoptic, Blocadren)
Non-Selective B ANTagonist

Uses:
1) Topically in eye for Glaucoma (decreased aqueous humor production). Does NOT cause Miosis (pupil constriction)
2) Antihypertensive Drug
3) Antiarrhythmic Drug
Pindolol
Non-Selective B ANTagonist with Intrinsic Sympathomimetic Activity (Partial Agonist)

May produce Smaller reductions in HR than other B Antagonists

Uses:
1) Treatment of Hypertension in patients with significant Decreases in Cardiac Reserve or with a propensity for Bradycardia
Carvedilol (CoReg)
Major Drug for Congestive Heart Failure (CHF)

Used in Combo with ACE Inhibitors and Diuretics

Mx:
1) Pan B Blocker Activity
2) A1 Blocker
3) Anti-Oxidant Action
Metoprolol (Lopressor)
Prototype Selective B1 ANTagonist - "Cardioselective B Blocker"

Uses:
1) Hypertension

Side Effects:
1) used with caution in Pts with Asthma, COPD, Etc.
2) Cardiac Decompensation in patients with borderline heart failure
Atenolol (Tenormin)
B1 ANTagonist

Uses:
1) Antihypertensive Agent
Reserpine
Neuronal Blocking Agent - Selective and Irreversible Inhibition

Plant Alkaloid

Blocks Noradrenergic Neuronal Vesicle Amine Transport Mx

Uses:
1) Hypertension