BACLOFEN

ACTION

GABA-B receptor agonist. Its beneficial effects in spasticity result from actions at spinal and supraspinal sites. Blocks mono-and-polysynaptic reflexes by acting as an inhibitory neurotransmitter, blocking the release of excitatory transmitters.

INDICATIONS

Spasticity: Start 5 mg orally three times daily, increase every 3 days to 20 mg orally three times daily. Max dose: 20 mg orally four times daily (80mg/day).
Hiccups (unlabeled use): 10-20 mg 2-3 times/day.

COMES AS

Injection (soln) intrathecal [preservative free] (Lioresal®):

50 mcg/mL (1 mL)

500 mcg/mL (20 mL)

2000 mcg/mL (5 mL).

Tablet: 10 mg, 20 mg


DOSAGE

Intrathecal:

  • Test dose: 50-100 mcg, doses >50 mcg should be given in 25 mcg increments, separated by 24 hours.
  • A screening dose of 25 mcg may be considered in very small patients.
  • Patients not responding to screening dose of 100 mcg should not be considered for chronic infusion/implanted pump.
  • Maintenance: After positive response to test dose, a maintenance intrathecal infusion can be administered via an implanted intrathecal pump. Initial dose via pump: Infusion at a 24-hourly rate dosed at twice the test dose. Avoid abrupt discontinuation.

BENDFROFLUMETHIAZIDE

 

ACTION

Bendroflumethiazide is a thiazide diuretic. These act mainly on the early segment of the distal tubule by inhibiting Na+ and Cl reabsorption. This leads to increased Na+ and Cl excretion and therefore increased water secretion.

INDICATIONS

  • Hypertension
  • Oedema caused by cardiac failure
  • Oedema caused by diabetes insipidus

COMES AS

  • PO
    • 5mg and 5mg tablets.

DOSAGE

  • For oedema
    • Initially 5-10mg once daily or on alternative days, dose to be taken in the morning, then maintenance 5-10mg 1-3 times a week.
  • For hypertension
    • 5 mg daily, dose to be taken in the morning, higher doses are rarely necessary

 

WARNINGS AND PRECAUTIONS

  • Hypersensitivity to Bendroflumethiazide or other sulphonamides
  • Hypokalaemia can occur with both thiazide and loop diuretics. The risk of hypokalaemia depends is greater with thiazides than with an equipotent dose of a loop diuretic
  • Cirrhosis (risk of development of hepatic encephalopathy)
  • Thiazides and related diuretics can exacerbate diabetes, gout, and systemic lupus erythematosus.
  • Lower initial doses of diuretics should be used in the elderly because they are particularly susceptible to the side-effects.
  • RARE
    • Agranulocytosis, blood disorders, impotence, leucopenia, thrombocytopenia

 

BENZYLPENICILLIN

 ACTION

Penicillins contain a b-lactam ring fused with a thiazolidine ring. Penicillins are bactericidal antibiotics that inhibit cell wall synthesis. When gram-positive bacteria are exposed to b-lactams, growth continues but with reduced cross-linkage of peptidoglycan resulting in weakening of the cell wall and lysis.

INDICATIONS

  • Gram +ve cocci
  • Meningococcal infections
  • Mild-moderate susceptible infections
  • Throat infections
  • Otitis Media
  • Cellulitis
  • Pneumonia
  • Endocarditis
  • Anthrax (in combination with other antimicrobials)
  • Intrapartum prophylaxis against group B streptococcal infection

COMES AS

  • IV/IM
    • 600mg and 1.2g powder for solution for injection vials. Dissolve in at least 8mL of water for injection

 


DOSAGE

For pneumonia

By IM, or by slow IV injection, or by intravenous infusion. 0.6–1.2 g every 6 hours, dose may be increased if necessary in more serious infections, single doses over 1.2 g to be given by intravenous route only.

For endocarditis

By slow IV injection, or by intravenous infusion. 1.2g every 4 hours, increased if necessary to 2.4g every 4 hours, dose may be increased in infections such as enterococcal endocarditis.

For meningitis

By slow IV injection, or by intravenous infusion. 2.4g every 4 hours.


WARNINGS AND PRECAUTIONS

  • Hypersensitivity to Penicillins
  • Accumulation of sodium from injection can occur with high doses

COMMON

  • Anaphylaxis, angioedema, diarrhoea, fever, hypersensitivity reactions, joint pains, rashes, serum sickness-like reaction, urticaria

RARE

  • Cerebral irritation, CNS toxicity (including convulsions), coagulation disorders, encephalopathy, haemolytic anaemia, interstitial nephritis, leucopenia, thrombocytopenia

 

BISOPROLOL

ACTION

Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol competitively blocks the β1-adrenoceptor thus blocking the activation of the signalling cascade which is normally activated by adrenaline and noradrenaline stimulation. This decreases the adrenergic tone of the heart and pacemaker cell activity.

INDICATIONS

  • Myocardial infarction
  • Heart failure
  • Angina
  • Hypertension

COMES AS

  • PO
    • 25mg, 2.5mg, 3.75mg, 5mg, 7.5mg and 10mg tablet

DOSAGE

For angina

  • 5–10 mg once daily; maximum 20 mg per day.

For adjunct in heart failure

  • By Initially 1.25 mg once daily for 1 week, dose to be taken in the morning, then increased if tolerated to 2.5 mg once daily for 1 week, then increased if tolerated to 3.75 mg once daily for 1 week, then increased if tolerated to 5 mg once daily for 4 weeks, then increased if tolerated to 7.5 mg once daily for 4 weeks, then increased if tolerated to 10 mg once daily; maximum 10 mg per day.

WARNINGS AND PRECAUTIONS

  • Hypersensitivity to Bisoprolol
  • Contraindicated in patients who suffer from bronchospasm
  • Contraindicated in: Asthma, cardiogenic shock, hypotension, marked bradycardia, metabolic acidosis, phaeochromocytoma (apart from specific use with alpha-blockers), Prinzmetal’s angina, second-degree AV block, severe peripheral arterial disease, sick sinus syndrome, third-degree AV block, uncontrolled heart failure
  • Acute or decompensated heart failure requiring intravenous inotropes, sino-atrial block

UNCOMMON

  • Cramp, depression, muscle weakness

RARE

  • Dry eyes, hypertriglyceridaemia, hearing impairment, syncope

 

Section Editor: Dr Paul Efthymiou