Exam 4: Adrenergic Antagonists Flashcards
What is chemical class and USAN stem of a1 antagonist?
Quinazolines and azosin
What are examples of selective a1 antagonist?
- Prozaosin
- Terazosin
- Doxazosin
- Tamsulosin
- Alfuzosin
- Silodosin
How does a2 antagonist differ from a1?
Can cause mimetic action due to a2 being and autoreceptor
What is yohimbine’s characteristics?
- Not clinically significant
- Induces hypertension
- Increases heart heat
- Male impotence and orthostatic hypotension
What are the therapeutic effects of b1 antagonists?
Reduce contractile force and heart rate lowering BP
What are the categories of b antagonists?
Aryloxypropanolamines
Arylethanolamines
What is the USAN for beta blockers?
Aryloxypropanolamines: olol
Arylethanolamines: alol
What is the Aryloxypropanolamines B1 antagonist SAR?
- Catechol ring can be replaced by wide variety of aromatic rings
- OH group essential
- Most marketed as (+) but b-blockade due to (S) (-)-configuration
- Bulky N-substituents confer b-receptor selectivity
What is used to treat glaucoma?
B-blockers such as
Timolol (Timoptic), Betaxolol (Betoptic), Levobunolol (Betagan), Metipranolol (Optipranolol), Carteolol (Ocupress)
How should beta blockers be used to treat antihypertensives?
b1-selectivity important for ‘clean’ hypertension treatment
Why is selectivity important?
Increased side effects by increasing the site of action
What are the common ADRs of non-selective B-blockers?
- Temporary fatigue
- Bronchoconstriction
- Sexual dysfunction
- Arrhythmias
What are the B1-selective antagonists?
BEAM-N
1. Acetbutolol
2. Atenolol
3. Betaxolol
4. Bisoprolol
5. Esmolol
6. Metoprolol
7. Nebivolol
What are the B1-non selective antagonists?
Metopranolol
What is the receptor specificity of propranolol?
B1 and 2
What is the therapeutic use for propranolol?
- Hypertension
- Migraine
- Hyperthyroidism
- Angina pectoris
- Myocardial infarction
What is the receptor specificity of Nadolol?
B1 and 2
What is the therapeutic use for Nadolol?
Hypertension
What is the receptor specificity of timolol?
B1 and 2
What is the therapeutic use for timolol?
Glaucoma and hypertension
What is the receptor specificity of acebutolol, atenolol, esmolol, and metoprolol?
B1
What is the therapeutic use for acebutolol, atenolol, esmolol, and metoprolol?
Hypertension
What is the receptor specificity of nebivolol?
B1 and Nitric oxide increase
What is nebivolol’s therapeutic use?
Hypertension
