66 - Beta blockers

*Beta blockers are drugs which act against the beta adrenergic receptors. There are three kinds of adrenergic receptors namely beta1, beta2 and beta3.

*First generation beta blockers (non-selective beta blockers) :
- Propranolol
- Nadolol
- Timolol
- Penbutalol
- Pindolol
- Oxprenolol
- Alprenolol

*Second generatin beta blockers ( Beta1 selective beta blockers = Cardioselective beta blockers ):
- Acebutalol
- Celiprolol
- Bisoprolol
- Metaprolol
- Nebivolol (most cardioselective beta blocker)
- Atenolol
- Esmolol
- Betaxolol

*Third generation beta blockers ( These are beta blockers which have additional vasodilator property ):
- Labetalol and Carvedilol ( act as vasodilators by antagonising alpha1 receptors on blood vessels)
- Tilosolol ( act as vasodilator by opening up potassium channels)
- Nebivolol and Nipradilol ( generate Nitric oxide )
- Bevantolol, Betaxolol, Carvedilol ( inhibit calcium channels )
- Bopindolol, Carteolol, Celiprolol ( agonists of beta2 receptors )

* Beta blockers with Membrane stabilising activity (local anaesthetic activity) :
- Propranolol (most effective)
- Labetalol
- Acebutolol
- Metaprolol
- Pindolol

* Beta blockers with intrinsic sympathomimetic activity :
- Oxprenolol
- Alprenolol
- Pindolol
- Celiprolol

* Beta blockers which are lipid insoluble ( so they are excreted by kidney and hence contraindicated in renal failure - LONG ACTING AGENTS ) :
- Nadolol
- Sotalol
- Acebutalol
- Atenolol
- Betaxolol
- Bisoprolol
- Celiprolol

* Longest acting beta blocker is Nadolol
* Shortest acting beta blocker is esmolol.

65 - Drugs causing CYP3A inhibition

1. HIV antivirals : Indinavir, nelfinavir, ritonavir, Saquinavir
2. Clarithromycin
3. Itraconazole and Ketaconazole
4. Nefazodone
5. Telithromycin
6. Aprepitant
7. Erythromycin
8. Grapefruit juice
9. verapamil, diltiazem
10. Cimetidine
11. Amiodarone
12. Chloramphenicol
13. Ciprofloxacin
14. Delaviridine
15. Diethyl-dithiocarbamate
16. fluvoxamine
17. gestodene
18. Imatinib
19. Mibefradil
20. Mifepristone
21. Norfloxacin
22. Norfluoxetine
23. Starfruit
24. Voriconazole