Rodriguez Adrenergic antagonists Flashcards
What reactions do B1 adrenoreceptors do?
1) tachycardia
2) increased myocardial contractility
3) increased lipolysis
What do B2 adrenorecptors do?
1) Vasodilation
2) slight decrease in peripheral resistance
3) bronchodilation
4) increased glycogenolysis ( liver and muscle)
5) increased Glucagon release
6) relaxation of uterine smooth muscle
How is the ciliary body effected by post-ganglionic sympathetic activity?
1) There are mainly B2 receptors in the stroma and epithelia of ciliary body.
2) there are a2 recpetors at eh non-pigmented epithelium
3) adrenergic stimulation causes ciliary muscle relaxation -but is not clinically significant.
4) a receptor stimulation at the non-pigmented epithelium produces an inhibitory response, causing a decrease in aqueous production
What are B adrenoreceptor antagonists?
1) b blockers
2) inhibit catecholamines reversibly
3) cardio selective
4) ocular hypotensive drug
How do B blockers work?
block the production of aqueous humor on non pigmented epithelium.
Also causes vasoconstriction on CB vessels.
Timolol Maleate
non-cardioselective b-blocker
2) negative sympathomimetic activity
3) concentrations come in 0.25% and 0.5%
What does Timolol maleate act on?
the ciliary body
> B2 adrenoreceptors and some B1.
How much does Timolol decrease IOP by?
20-30%
Aprox: 7mmHg
Timolol administration
1 drop BID or 1 drop d
Max effect achieved after 3 weeks.
It has a contralateral effect.
must be applied in the morning.
Clinical uses of Timolol
1) Primary Open angle glaucoma.
2) Ocular hypertension
3) Pre and Post surgery
What is an ocularhypotension drug that can be used before and after surgery?
timolol
What are the OCULAR side effects of Timolol
1) Blepharo conjunctivitis : Erythema and edema
2) Decreased corneal sensitivity
3) Dry Eye: Superficial punctate keratopathy
What are the systemic side effects of Timolol?
– Bradycardia – Systemic hypotension – CHF – Heart block – Bronchospasm – Diarrhea – Amnesia – Elderly special consideration – Hypoglycemia – Alteration lipid plasma profile
Contraindications of TImolol
- Bronchial asthma
- COPD
- Bradycardia
- Severe heart block
- Overt Cardiac Failure
- Children and infants