Pharm: Adrenergic Drugs

Front 1

ALBUTEROL
TERBUTALINE
Metaproterenol

Back 1

RECEPTOR: B2

PHYSIOLOGICAL AXN(s): bronchodilation

THERAPEUTIC USES:
- treatment of bronchospasm/asthma
- chronic abstructive pulmonary disease
- bronchitis
- terbutaline can be used to relax the uterus during premature labor

ADVERSE EFX:
arrythmias
tachycardia
headache
nausea and vomiting

* albuterol is usally inhaled; terbultaline is usually given orally or subcutaneously

Front 2

PHENYLEPHRINE

Back 2

RECEPTOR: a1

PHYSIOLOGICAL AXN(s): vasoconstriction

THERAPEUTIC USES:
- nasal decongestant
- for occular examinations to induce mydriasis
- often injected w/ a local anesthetic to cause vasoconstriction

ADVERSE EFX:
rebound mucousal swelling
hypertensive headache

Front 3

AMPHETAMINE

Back 3

RECEPTOR: a, B, CNS

PHYSIOLOGICAL AXN(s): releases stores of epinephrine and dopamine; it can enter the CNS

THERAPEUTIC USES:
- treatment of ADHD
- appetite suppression
- narcolepsy

ADVERSE EFX:
psychological and physical dependence
psychosis, confusion, resltessness
insomnia
headache
palpitations
tachycardia
impotence

Front 4

CLONIDINE

Back 4

RECEPTOR: a2

PHYSIOLOGICAL AXN(s):
reduces sympathetic NS outflow from the brain

THERAPEUTIC USES:
- treatment of Hypertension

ADVERSE EFX:
sedation
dry mouth
sexual dysfunction
orthostatic hypotension

Front 5

DOBUTAMINE

Back 5

RECEPTOR: B1 (some known B2 activity)

PHYSIOLOGICAL AXN(s):
increased heart rate and contractility(B1)
smooth muscle relaxation (B2)

THERAPEUTIC USES:
- treatment of congestive heart failure CHF and shock

ADVERSE EFX:
arrythmias
headache
hypertension
palpitations
angina
nausea

* a dopamine analog; administered by IV

Front 6

ISOPROTERENOL

Back 6

RECEPTOR: B1, B2

PHYSIOLOGICAL AXN(s):
- increased cardiovascular ionotropic and chronotropic response (B1)
- lowers PVR
- relaxes smoothe mucles

THERAPEUTIC USES:
- cardiac stimulant in pts with heart block and bradycardia

ADVERSE EFX:
arrythmias
palpitations
tachycardia
headache

* administered by IV; in the past it was used to treat asthma

Front 7

METHOXAMINE

Back 7

RECEPTOR: a1

PHYSIOLOGICAL AXN(s): vasoconstriction

THERAPEUTIC USES:
- treatment of hypotension and PAT
- supraventricular tachycardia

ADVERSE EFX:
rebound mucousal swelling
hypertensive headache

* non Catecholamine - compared to chatecholamines has a longered duration of action and can be administered orally

Front 8

EPHEDRINE

Back 8

RECEPTOR: a, B, CNS

PHYSIOLOGICAL AXN(s):
direct adrenergic agonist; stimulates release of norepineprhine from nerves

THERAPEUTIC USES:
- urinary incontinence
- bronchospasm
- hypotension

ADVERSE EFX:
arrythmias
palpitations
insomnia
hypertension

* an alkaloid that can be given orally; has prolonged stimulant effects on the CNS

Front 9

NOREPINEPRHINE

Back 9

RECEPTOR: a1, a2, B1

PHYSIOLOGICAL AXN(s): vasoconstriction

THERAPEUTIC USES:
- last line agent in the treatment of shock

ADVERSE EFX:
tissue hypoxia b/c potent vasoconstriction
decreased kidney perfusion
arrythmias
tissue necrosis

Front 10

CATECHOLAMINES

Back 10

Epineprhine
Norepineprhine
Isopreterenol
Dopamine
Dobutamine


PHARMACOLOGIC CHARACTERISTICS:
- sypathomimetic amines that contain the 3,4- dihydroxybenzene group
- high potency; rapid onset w/ breif duration of action
- not administered orally
- poor penetration into the CNS

Front 11

NON-CATECHOLAMINES

Back 11

Phenylephrine
Methoxamine
Clonidine
Albuterol, Terbutaline
Amphetamine
Ephedrine

PHARMOCOLOGIC CHARACTERISTICS:
- compounds lacking the catechol hydroxyl group
- longer half lives, longer duration of action
- all can be administered orally

Front 12

PRAZOSIN
Terazosin
Doxazosin

Back 12

RECEPTOR: a1 blockers

PHYSIOLOGICAL AXN(s):
- relaxation of SM tone in bladder
- inhibits constricion of vascular SM --> decreased PVR and lower BP

THERAPEUTIC USES:
- hypertension
- preventionof urinary retention in pts with benign prostatic hypertrophy

ADVERSE EFX:
GI hypermobility
Orthostatic HT
sexual dyxfunction, drymouth, dizziness

Front 13

PHENOXYBENZAMINE

Back 13

RECEPTOR: a blocker

PHYSIOLOGICAL AXN(s):
blocks peripheral vasoconstriction and induces reflex tachycardia

THERAPEUTIC USES:
- pheochromocytoma induced HT
- benign prostatic hypertrophy, reduces size of prostate
- hyperreflexia due to spinal cord injuries
- Raynauds disease

ADVERSE EFX:
orthostatic hypotension, reflex tachycardia, sexual dysfunction

* administered orally; drug has a very long duration of action

Front 14

PHENTOLAMINE

Back 14

RECEPTOR: a blocker

PHYSIOLOGICAL AXN(s):
reversibly blocks a1 an a2 receptors

THERAPEUTIC USES:
short term control of pheochromocytoma induced HT

ADVERSE EFX:
Orthostatic hypotension
GI stimulation leading to peptic ulcers
tachycardia, MI, arrythmias

* administered IV or IM, poorly absorbed orally; half-life 4 hours

Front 15

MIRTAZAPINE

Back 15

RECEPTOR: a2 receptors

PHYSIOLOGICAL AXN(s):
blocks presynaptic a2 receptors and facilitates release of norepinephrine

THERAPEUTIC USES:
antidepressant

ADVERSE EFX:
unknown

* NEW, FDA just approved for use

Front 16

PROPANOLOL

Back 16

RECEPTOR: B blocker

PHYSIOLOGICAL AXN(s):
antogonizes the efx of catecholamines on all B receptors
- negative inotropic and chronotropic efx on heart
- slows atrioventricular conduction
- promotes bronchoconstriction

THERAPEUTIC USES:
Hypertension
Angina, Tachycardia
Myocardial Infarction
Cardiac Arrythmia

ADVERSE EFX:
contraindicated in asthmatics
fatigue, depression, sexual dysfunction

Front 17

LABETALOL

Back 17

RECEPTOR: non selective B blocker; a1 blocker

PHYSIOLOGICAL AXN(s):
peripheral vasodilations

THERAPEUTIC USES:
hypertension
atrial fibrillation

ADVERSE EFX:
orthostatic hypotension
dizzines

Front 18

ATENOLOL
METOPROLOL

Back 18

RECEPTOR: B1 blocker

PHYSIOLOGICAL AXN(s):
cardioselective bronchoconstiction

THERAPEUTIC USES:
Atenolol - Hypertension, MI
Metoprolol - HT, anginal pain, myocardial infarction

ADVERSE EFX:
hypotension
bradycardia
fatigue
drowsiness

Front 19

GUANETHIDINE

Back 19

RECEPTOR: Indirect Adrenergic Antagonist

PHYSIOLOGICAL AXN(s):
- enters the peripheral adrenergic nerve by a reuptake mechanism for NE
- concentrates in storage vesicles replacing NE and causes gradual depletion of NE stores
- interrupts transmission of impulses btwn sympathetic neurons and effector organs

THERAPEUTIC USES:
Severe Hypertension

ADVERSE EFX:
orthostatic hypotension
sexual dysfunction
very prolonged action

Front 20

TIMOLOL
nadolol

Back 20

RECEPTOR: non selective B antagonist

PHYSIOLOGICAL AXN(s):
reduces production of aqueous humor in the eye

THERAPEUTIC USES:
- topically in treatment of open angle glaucoma
- systemic treatment of HT (rarely)

ADVERSE EFX:
contraindicated in asthma patients