Antiadrenergic Drugs Part 2 - Dr. Konorev Flashcards
Direct Antiadrenergic drugs
- A adrenoreceptor antagonist
- non-selective (a1 and a2)
- a1 selective - Mixed blockers (B and a1)
- B adrenoreceptor blockers
- B1 and B2
- B1 selective
Indirect Antiadrenergic drugs
- NE release inhibitor
2. Tyrosine Hydroxylase inhibitor
Non-selective a1 and a2 receptor antagonist
2
- Phenotolamine
2. Phenoxybenzamine
A1 selective R antagonist
3
- Prazosin
- Tamsulosin
- Doxazosin
Mixed blockers
2
- Labetalol : B and a1 antagonist
2. Carvedilol : B and a1 antagonist
B R blockers : B1 and B2
3
- Propranolol
- Pindolol
- Ndolol
B R blockers : B1 selective
4
- Metoprolol
- Betaxolol
- Acebutolol
- Atenolol
NE release inhibitor
1
Guanethidine
Tyrosine Hydroxylase inhibitor
1
Metyrosine = inhibit synthesis of NTs
Phentolamine what type of drug and HL
Reversible competitor , non-covalent binding
Short half life
You can reverse by giving antagonist to it
Phenoxybenzamine type of drug and HL
Non-competitive irreversible , covalent binding
Longer H
Miosis
Pupil constriction (pupil dilator muscle relaxes)
Most seen thing in a antagonist effect
Lower BP
= can cause Tachycardia as body responds
TX phenochromocytoma ( adrenal gland tumor, making catecholamines)
Phentolamine, phenoxybenzamine, metyrosine
TX Chronic HTN
Prazosin, doxazosin (a1 selective)
TX erectile dysfunction
Phentolamine + vasodilator
TX benign prostate hyperplasia (BPH)
= treats chronic urinary obstruction (incontinence)
Tamsulosin (A1a)——> prevent prostate SM contraction without decrease in BP
Some adverse effects of a antagonist drugs
Tachy Nasal stuffiness Postural hypotension = body response Fluid retention = body response X ejaculation
B1 selective antagonist other name
Cardiac selective
= heart has B1 only
Antagonists B blockers
Atenolol
Nadolol
Propranolol
Partial antagonist B blockers
Acebutolol
Labetalol
Pindolol
Inverse agonists
Betaxolol
Metoprolol
Partial Agonist : beta-blockers use and other name
ISA : Intrinsic Sympathomimetic activity B-blockers
= good for pt who has HTN + low HR, this drug can decrease BP and not have as much decrease on HR
Beta blockers main effects
Heart
BVs
Kidney
- Slow HR , force and AV conduction
- Initially increase BV constriction and then decrease it when long-term use
- Inhibits renin release
Beta blockers main effects
Lungs
Eye
metabolism
- Increase airway resistance
- Reduce aqueous humor = lower intraocular pressure
- X lipolysis, increase VLDL, X glycogenolysis + gluconeogenesis
5 conditions Beta-blockers are used for heart related
- Chronic HTN
- Angina Pectoris
- MI
- Cardiac Arrhythmia (ventricular and supraventricular, atrial fib or flutter, V ectopic beats)
- Heart Failure : Metoprolol and carvedilol (not for congestive HF)
2 conditions Beta-blockers are used for NOT heart related
- Glaucoma : Betaxolol (also has anesthetic activity)
2. Hyperthyroidism : Propranolol
B1 2 main functions
Increase HR and increase RENIN
Adverse effects of B-blockers 5 and what to do
- CNS effects : depression, sleep problems (switch to most hydrophilic drug)
- Resp bronchospasm or asthma, airway resistance (switch to B1 selective)
- Cardiac depression (switch to partial antagonist)
- Low cholesterol from decrease in HDL (switch to partial antagonist)
- Hypoglycemia in DM (switch to B1 selective)
Abrupt discontinuation of B-blockers can cause what
Cardiac problems from sympathetic hyper-responsiveness =arrhythmia , ischemic heart disease,
= during drug of B-blocker ——> body compensated by increasing B receptors on the neurons ——> super stimulation when drug is removed
