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Beta - blockers


  1. Non-selective (beta 1= beta 2)
    1. Propanolol                        
    2. Sotalol                  
    3. Nadolol
    4. Timolol                    
    5. Levobunolol


  1. Selective/ First generation (beta1 >> Beta 2)
    1. Atenolol                          
    2. Metoprolol                  
    3. Bisoprolol
    4. Betaxalol                        
    5. Esmolol


  1. Non Selective/ third generation ( beta1=beta 2)
    (ISA with additional cardiovascular action)
    1. Alprenolol                
    2. Oxprenolol          
    3. Pindolol        
    4. Celiprolol     
    5. Carteolol                
    6. Acebutolol            
    7. Penbutolol


  1. Combined (Alpha-1, beta-1>> beta-2)
    Additional cardiovascular action
    1. Carvedilol        
    2. Dilevelol            
    3. Labetalol              
    4. Bucindolol    
    5. ​Nebivelol


  1. Beta-2 blocker

a.  Butoxamine




  1. Beta blockers are of two types
  2. Lipid soluble (MP3-Metoprolol, propanolol, pindolol, penbutolol)
  3. Water soluble (ANS-Atenolol, nadolol, sotalol)
  4. Shortest acting-esmolol
    1. Concentrates in RBCs            
    2. Metabolised by estereases
    3. Half life-10-20 mins            
    4. Safe in hepatic & renal failure  
    5. Nadolol-longest acting, half life=24 hours, accumulated in renal failure-C/I
    6. Propanolol is maximally lipid soluble-highest hepatic first pass-C/I
    7. Atenolol has minimum protein binding (5%)
    8. Propanolol has high protein binding (90%)
    9. Metoprolol-maximum inter-individual variation  

Additional cardiovascular action:

Beta Receptor Antagonists with Additional Cardiovascular Actions: Proposed Mechanisms Contributing to Vasodilation

Nitric Oxide Production

Beta-2 Receptor Agonism

Apha-1 Receptor Antagonism

Ca2+ Entry blockade

KChannel opening

Antioxidant activity








Drug Actions

  1. Brain
    1. Useful (Antihypertensive, antianxiety)
    2. Harmful (Hallucinations, depression, insomnia-decrease in melatonin)
    3. Melatonin is used in jet lag, shift work insomnia
    4. Ramelteon is melatonin receptor agonist, used for initial insomnia
  2. Eye
    1. Reduce formation of aqueous humor
    2. Anti-glaucoma activity
    3. Even topical beta-blockers can have systemic effects via nasolacrimal absorption
  3. Bronchi
    1. Bronchospasm
    2. Cardio-selective beta blockers are safe in asthma
    3. CCBs are safe in asthma, diabetes & CHF
  4. Heart
    1. Decrease heart rate---decrease O2 requirement---antianginal activity
    2. Decrease cardiac output---antihypertensive action
    3. Membrane stabilizing activity-antiarrhythmic activity (PALM)
    4. Cardioprotective-CHF, AMI     


  1. Antihypertensive              
  2. Lipid lowering              
  3. Anti-platelet

Cardio protection in CHF

  1. Arrhythmias are major cause of death in CHF
  2. Beta-blockers, prevent arrhythmias, reduce mortality

American College of Clinical Cardiology Guidelines’ 2003 guidelines for use of beta blockers in CHF

  1. Low dose of beta blockers
  2. Use them in mild to moderate patients (NYHA I, II)
  3. Short duration
  4. Carvedilol or metoprolol
  5. Cardedilol is favored as it is an antioxidant

f.    No beta-blocker in severe heart failure

  1. Liver
    1. Inhibit glycogenolysis                
    2. Produce hypoglycemia        
    3. “Silent/masked”  
  2. Pancreas
    1. Reduce release of insulin          
    2. Can produce diabetes
  3. Skeletal muscles
    1. Antitremor action (Partial agonists have no antitremor action)
      1. Also have no usefulness in prophylaxis of migraine
      2. No anti-anginal activity
    2. Inhibit K+ uptake-hyperkalemia
    3. Reduce blood flow to skeletal muscles-fatigue, cold extremities
    4. Reduced exercise capacity   
  4. Lipid metabolism (hyperlipidemia)
    1. Activate tissue lipase                
    2. Increase VLDL            
    3. Total cholestrol
  5. Genito-urinary system
    1. Reduce blood flow to plaventa-IUGR         
    2. Reduce blood flow to penis-impotence-labetalol is maximally likely



  1. Propanolol (DOC)        
    1. Essential tremors
    2. Prophylaxis of migraine (Sodium valroate is an alternative-topiramate-refractory patients)
    3. HOCM                      
    4. Social phobia                          
    5. Toxic multinodular goiter    
    6. Aortic dilation in marfan                                 
    7. Intraoperative tachycardia
  2. Timolol (DOC)
    1. Primary open angle glaucoma        
    2. S/e-blepharoconjunctivitis
    3. Can have systemic effects
      1. Hypoglyecemia          
      2. Bradycardia          
      3. Impotence
  3. Betaxalol is used for glaucoma with asthma
  4. Labetalol
    1. Isomeric drug            
    2. Alpha+beta blocker            
    3. DOC

Aortic dissection (Past DOC-trimethophan which is a ganglion blocker)



C/I of beta blockers

  1. Diabetes          
  2. PVD            
  3. Asthma                
  4. COPD          
  5. Pregnancy            
  6. CHF              
  7. Heart block


  1. Glaucoma is a group of diseases characterized by a progressive form of optic nerve damage.
  2. This is generally associated with raised (> 21 mmHg) intraocular tension (i.o.t).
  3. The chief therapeutic measure is to lower i.o.t. to target Ievel, either by reducing secretion of aqueous humor or by promoting its drainage.
  4. Major amount of aqueous (-90%) drains through the trabecular route, while -10% fluid passes into the connective tissue spaces within the ciliary muscle then via suprachoroid into episcleral vessels (uveoscleral outflow).
  5. Glaucoma is seen in two principal clinical forms:

Open angle (wide angle, chronic simple) glaucoma

Angle closure (narrow angle, acute congestive) glaucoma

It is probably a genetically predisposed degenerative disease affecting patency of the trabecular meshwork, which is gradually lost past middle age.

The i.o.t. rises insidiously and progressively.

Ocular hypotensive drugs are used on a long-term basis and constitute the definitive treatment in majority of cases.


It occurs in individuals with a narrow irido-corneal angle and shallow anterior chamber. The i.o.t. remains normal until an attack is precipitated, usually by mydriasis.

The i.o.t. rises rapidly to very high values (40-60 mmHg).

It is an emergent condition; failure to lower i.o.t. quickly may result in loss of sight.


1. Beta Blockers - Timolol, Betaxolol, Levobunalol

2. Alpha agonist- Adrenaline, Depevefrine, Apraclonidine, Brimonidine

3. Prostaglandin analogues- Latanoprost

4. Carbonic anhydrase inhibitors- Acetazolamide, Dorzolamide, Brinzolamide

5. Miotics- Pilocarpine


Drugs are used only to terminate the attack of angle closure glaucoma.

1. Hypertonic mannitol (20%) 1.5-2g/kg or glycerol (10%) infused i.v. decongest the eye by osmotic action. A retention enema of 50% glycerine is also sometimes used.

2. Acetazolamide: 0.5 gm i.v. followed by oral twice daily is started concurrently.

3. Miotic: Once the i.o.t. starts falling due to the above i.v. therapy, pilocarpine 1-4 % is instilled every 10 min initially and then at longer intervals. Contraction of sphincter pupillae changes the direction of forces in the iris to losen its contact with the lens and spreads the iris mass centrally + pupillary block is removed and iridocorneal angle is freed. However, when i.o.t. is very high the iris muscle fails to respond to miotics; tension should be reduced by other measures before miotics can act.

4. Topical Beta blocker: Timolol 0.5% is instilled 1hourly in addition.

5. Apraclonidine (7%)/ Latanoprost 0.005%, instillation may be added

6. Definitive treatment is surgical or laser iridotomy.


Golden Points

Autonomic Nervous System

  1. Botulinum toxin reduces release of acetylcholine used in spasmodic disorders of muscles. 
  2. Acetylcholine is metabolized by true (neuronal enzyme) & false pseudocholinesterase (deficiency causes apnea)
  3. Bethanechol (direct acting cholinomimetic) is used in Hirsprung’s disease, achalasia cardia and post-operative urinary retention
  4. Neostigmine is DOC for post-operative recovery from non-depolarizing blockers, cobra bite and myasthenia gravis
  5. DOC for organophosphate poisoning is atropine; cholinesterase re-activators e.g. pralidoxime, obidoxime can also be used
  6. Atropine is C.I. in amanita muscaria poisoning
  7. Glycopyrrolate is atropine substitute specially useful for older patients undergoing surgery as it is more cardiostable. It is a tertiary amine and does not enter blood brain barrier as it is a quarternary amine. 
  8. Pipenzolate is used for infantile colic, while flevoxate is used for ureteric colic
  9. Hyosine butylbromide (Buscopan) is used commonly as anticholinergic drug for abdominal pain of spasmodic type
  10. Dicyclomine has both antiemetics and anti-motion sickness property
  11. Hyoscine (levo-scopolamine) is DOC for motion sickness and has amnesic properties (was used post world war-2 to produce amnesia)
  12. Adrenaline is DOC for angioedema, anaphylactic shock, cardiac arrest. It reduces formation of aqeous humor and increases aqueous humor (main mechanism).
  13. Isoproteranol is DOC for heart block (Causes pure rise of systolic BP) and also for torsa de depointes.
  14. Mephenteramine is DOC for short term rise of BP
  15. Dopamine is DOC for cardiogenic shock; acts on D1 receptors in kidney (renal vasodilator)
  16. Dobutamine (beta1 agonist-doesn’t act on dopamine receptors) is DOC for pump failure (e.g. following AMI, heart surgery)
  17. Phenyleprine is the drug that produces mydriasis without cycloplegia
  18. Midodrine is DOC for postural hypotension
  19. Methylphenidate is DOC for attention deficit hyperkinetic disorders
  20. Imipramine is DOC for nocturnal enuresis due to its anticholinergic property
  21. Ephedrine is DOC for hypotension induced by spinal anesthesia
  22. Alpha-blockers are of two types (selective & non-selective)
  23. Prazocin, terazocin are selective alpha1 blockers that do not cause reflex tachycardia as they don’t increase release of norepinephrine
  24. First dose hypotension is MC side effect of alpha blockers; they don’t increase lipid levels like beta-blockers-rather reduce them

Recent advances:  newer drugs


Tiotropium bromide (anticholinergic)

(COPD\ Chronic bronchitis\ emphysema)

Treprostinil (Prostaglandin analogue)

Pulmonary arterial hypertension
(PAH) in patients with NYHA Class II-IV symptoms

Botulinum toxin type A
(Inhibits Ach release)

Glabellar lines (cosmetic use) in adult men and women. Also used in Strabismus, (Blepharospasm, Cervical dystonia hemifacial spasms)

Vardenafil (PDS inhibitor )

Erectile dysfunction

Tadalafil (PD5 inhibitor )

Erectile dysfunction

Trovaprost (PG analogue)

Open – angle glaucoma or ocular hypertension

Dipivefrine (Adrenaline prodrug)


Matrifonate (Organophosphate)

Alzheimer’s disease

Solifenacin (Anticholinergic)

Unstable bladder

Darifenacin (Anticholinergic)

Unstable bladder

Trospium (Anticholinergic)

Unstable bladder

Tolterodine (Anticholinergic)

Unstable bladder (Drug of choice)

Cevemeline (Cholinergic)

Dry mouth, dry eyes (Sjogren syndrome) 


 Avanafil: Fastest acting PDE-5 inhibitors useful for the t/t of impotency. 

 Aclidinium bromide: Longest acting M3 receptor blocker approved for the T/t for COPD.

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