H2 BLOCKER

ADVERSE EFFECTS:

Less effective & less tolerated than PPI’s

Cimetidine:- Short duration of action; Enzyme inhibiror, increases plasma concentration of co-administrated drugs; Crosses BBB & produce CNS effects (confusion, headache, hallucinations); Increases plasma prolactin level, cause menstrual irregularities & galactorrhoea in women, gynaecomastia, oligospermia & impotence in men.

Other adverse effects:

Constipation, diarrhea, dry skin, tinnitus, nausea, vomiting etc.

REFERENCE:

Pharmacology 4th Ed: Tara V Shanbhag, Smita Shenoy

DAPSONE

It is a sulphone, oldest and cheapest ; most widely used for leprosy

MECHANISM OF ACTION

ADVERSE EFFECTS

Dose related hemolytic anemia in G6PD deficiency,

OTHERS: Anorexia, Nausea, Vomiting, Fever, Headache, Allergic dermatitis, Itching, Peripheral neuropathy, Methaemoglobin

Exacerbation of lesions- ‘ sulphone syndrome‘:- fever, dermatitis, pruritis, lymphadenopathy, methaemoglobinaemia, anemia, hepatitis

PHARMACOKINETICS

🟡 Given orally

🟡 almost completely absorbed from gut

🟡 bound to plasma proteins

🟡 widely distributed in in body and concentrated in infected skin, muscle, liver, kidney

🟡 partly secreted in bile and undergoes enterohepatic cycling

🟡 metabolized by acetylation and metabolites are excreted in urine

Reference:

Pharmacology 4th Ed: Tara V Shanbhag, Smita Shenoy