6 - Adrenergic Agonists & Antagonists Flashcards
What drug class/categorization?
Tamsulosin
indoramin / urapidil
Alpha Adrenergic Receptor ANTAGONIST
A1-Selective
What is
EPINEPHRINE REVERSAL?
Since Epi stimulates Both a-NE & b-NE receptors…
but the dominant effect = ↑BP
- *Alpha Effect (↑BP)**
- *OVERWHELMS**
- *B-NE effect** (Vasodilation -> ↓BP)
if EPI + a-NE ANTAGONIST are admin together –> lowered BP
What drug class/categorization?
EPINEPHRINE
ADRENERGIC AGONIST
Direct-Acting & A1/A2/B1/B2 non-selective
Catecholamine:
not orally, degraded by COMT & MAO
Beta Antagonist
Respiratory System Efects
Blockade of B2 Receptors in Bronchial Smooth Muscle:
↑Airway Resistance
Treatment of:
Angina / CHF following MI
Preferred are:
Selective B1 Antagonist = Metoprolol
What drug class/categorization?
Metoprolol** + **Esmolol
Beta Adrenergic Receptor ANTAGONIST
2st Gen = B1-Selective
What drug class/categorization?
Reserpine
NE ANTAGONIST
- *Inhibit VMAT2**
- depletes NT stores* –> ↓BP
not used often due to depression
What drug class/categorization?
Entacapone
ADRENERGIC AGONIST
Indirect Acting
COMT inhibitor
What Receptor?
Pancreatic Islets = INHIBITS Insulin Release
α2-Adrenoceptor Activation
found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells
liver cells / plateles / smooth muscles of BV’s & CNS neurons
What Receptor?
Externam Bladder Sphincter = Urine Retention
Genitilia = Ejaculation
α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION
What Receptor?
- *GI Tract & Smooth Muscle Walls = RELAXES**
- *(PRE-sympathetic Effect)**
α2-Adrenoceptor Activation
found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells
liver cells / plateles / smooth muscles of BV’s & CNS neurons
What drug class/categorization?
Bisoprolol** + **Betaxolol
B-Olol
Beta Adrenergic Receptor ANTAGONIST
B1-Selective
Bisoprolol = 2nd gen
Betaxolol = 3rd Gen
What drug class/categorization?
Selegiline
ADRENERGIC AGONIST
Indirect Acting
MAO inhibitor
What drug class/categorization?
Cocaine
ADRENERGIC AGONIST
Indirect Acting
- *Uptake Inhibitor**
- Impair re-uptake of release catecholamines into sympathetic neurons*
What drug class/categorization?
EPHEDRINE
ADRENERGIC AGONIST
Mixed Acting
A1/A2/B1/B2 & Releasing Agent
Non-Catecholamine:
resist MAO oxidation
What Receptor?
Sympathetic Nerve Terminals = INHIBITS NorEpinephrine Release
α2-Adrenoceptor Activation
found on BOTH :
PRE-synaptic neurons & POSTsynaptic cells
liver cells / plateles / smooth muscles of BV’s & CNS neurons
What drug class/categorization?
-ZOSINS
Prazosin / Terazosin / Doxazosin
Alfuzosin / Bnazosin
Alpha Adrenergic Receptor ANTAGONIST
A1-Selective
Without A2-NE Blockade:
less TachyCardia & Palpitations
What Receptor?
- *GI Tract**
- *Relax Muscular Motility**
α1-Adrenoceptor Activation
alpha 1 = more CONTRACTION
- *Adrenergic Agonist**
- *Catecholamine Properties**
Metabolism:
inactive derivatives are formed
mainly metabolized by Hepatic COMT , some in BRAIN
MAO for some NT’s released from vesicles in nerve terminal
NOT GIVEN ORALLY
IV / IM / Topical / Sprays
What Receptor?
Skeletal Muscle Cells = Tremor / Glycogenolysis (HYPERglycemia)
β2-Adrenoceptor Activation
B2 = more RELAXATION
What drug class/categorization?
Nadolol** / **Sotolol** / **Timolol“3-letter +olol, except for esmolol”
levobunolol / metipranolol
Beta Adrenergic Receptor ANTAGONIST
1st Gen = Non-Selective
What drug class/categorization?
Clonidine
ADRENERGIC AGONIST
Also Guanabenz
Direct-Acting & a2-Selective
↓BP
through central action ↓NE
What drug class/categorization?
Labetalol** + **Bucindolol
Beta Adrenergic Receptor ANTAGONIST
NON-Selective
3rd gen
What Receptor?
FAT CELLS = Lipolysis
TGs –> FFA’s
Fat Cells = THERMOGENESIS in skeletal muscle
β3-Adrenoceptor Activation
What drug class/categorization?
Yohimbine
Alpha Adrenergic Receptor ANTAGONIST
A2-Selective