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Hydroxy chloroquine (covid-19)

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DrRahulArya

- Hydroxychloroquine (HCQ) is an antimalarial drug that can be administered orally to treat conditions like malaria, lupus, and rheumatoid arthritis. - It is absorbed rapidly in the gastrointestinal tract, distributed widely in tissues, and eliminated mainly through the kidneys. The half-life is 32-50 days. - HCQ works by accumulating in lysosomes and increasing their pH. This blocks toll-like receptors on dendritic cells and reduces inflammation. - Potential side effects include nausea, diarrhea, skin rash, retinopathy, and cardiac issues. It can interact adversely with some medications like insulin, digoxin, and antacids. Overdose may

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HYDROXY-CHLOROQUINE [HCQ] Covid-19
HYDROXY-CHLOROQUINE • Class- Anti malarial drug • Trade name- plaquenil • Route of drug administration- Oral • Dose of drug- 200 mg [take as per directed by physician]
PHARMACO-KINETICS • Bioavailability- variable [average-74%] • Plasma Protein binding- 45% • Half life – 32-50 days • Matabolism – liver [ metabolize by enzyme cytrochrome p450] • Excretion- mostly by kidney <10% by biliary excretion • HCQ has similar pharmacokinetics to chloroquine with rapid gastrointestinal absorption and eliminated by kidney
PHARMACO-DYNAMICS • Anti malarial drugs are- (i) lipophilic, weak base (ii) easily pass plasma membrane HCQ is a weak diprotic base that can pass through the lipid cell membrane. The free base form accumulated in lysosomes and then protonated that results in increases the pH of lysosomes .
MECHANISM OF ACTION [MOA] • HCQ increases lysosomal pH in APCs • In inflammatory conditions, it blocks TLR (tall like receptors) on PDCs (plasmacytoid dendritic cells) • TLR-9 which recognizes DNA-containing immune complexes, leads to production of interferon and causes the dendritic cells to mature and present antigen to T-cells. • HCQ by decreasing TLR signaling, reduces the activation of dendritic cells and the inflammatory process.
USES OF HCQ • Prevention & treatment of malaria • SLE (systemic lupus erythematosus) • Rheumatoid arthritis • Q-fever • Porphyria cutanea tarda • Post lyme arthritis • Sjogren syndrome ( but less effective) • As of 3 April 2020 use of HCQ for corona virus disease (covid-19)
SIDE EFFECTS OF HCQ • Nausea , abdominal cramps , diarrhoea • Reduced appetite • Acne , anemia , skin rash • Loss of hair • Vertigo , convulsions • Eye pigmentation • Retinopathy (most dangerous side effect, can cause permanent vision loss)
OVERDOSE • Effects shows within an hour of ingestion • Sleepiness • Permanent vision loss • Seizure • Hypotension • Ventricular fibrillation • Respiratory failure
CONTRAINDICATION • Patient on anti arrhythmic medication because HCQ can prolong QT interval] • Psoriasis • Porphyria • Renal failure • Lactating mother (HCQ can enter breast milk) • children
DRUG INTERACTION • 1. [HCQ & Penicillamine]- increase plasma concentration of penicillamine, which may leads to severe side effects. 2. [HCQ & insulin]- enhances hypoglysemic effcts of insulin 3. [HCQ & antacids]- antacids may decrease the absorption of HCQ.
DRUG INTERACTIONS 4. [HCQ & neostigmine/pyridostigmine]- antagonize the action of HCQ. 5. [HCQ & digoxin]- increases serum digoxin levels 6. [HCQ & anti epileptics]- impaie the antiepileptic activity
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Hydroxy chloroquine (covid-19)

  • 2. HYDROXY-CHLOROQUINE • Class- Anti malarial drug • Trade name- plaquenil • Route of drug administration- Oral • Dose of drug- 200 mg [take as per directed by physician]
  • 3. PHARMACO-KINETICS • Bioavailability- variable [average-74%] • Plasma Protein binding- 45% • Half life – 32-50 days • Matabolism – liver [ metabolize by enzyme cytrochrome p450] • Excretion- mostly by kidney <10% by biliary excretion • HCQ has similar pharmacokinetics to chloroquine with rapid gastrointestinal absorption and eliminated by kidney
  • 4. PHARMACO-DYNAMICS • Anti malarial drugs are- (i) lipophilic, weak base (ii) easily pass plasma membrane HCQ is a weak diprotic base that can pass through the lipid cell membrane. The free base form accumulated in lysosomes and then protonated that results in increases the pH of lysosomes .
  • 5. MECHANISM OF ACTION [MOA] • HCQ increases lysosomal pH in APCs • In inflammatory conditions, it blocks TLR (tall like receptors) on PDCs (plasmacytoid dendritic cells) • TLR-9 which recognizes DNA-containing immune complexes, leads to production of interferon and causes the dendritic cells to mature and present antigen to T-cells. • HCQ by decreasing TLR signaling, reduces the activation of dendritic cells and the inflammatory process.
  • 6. USES OF HCQ • Prevention & treatment of malaria • SLE (systemic lupus erythematosus) • Rheumatoid arthritis • Q-fever • Porphyria cutanea tarda • Post lyme arthritis • Sjogren syndrome ( but less effective) • As of 3 April 2020 use of HCQ for corona virus disease (covid-19)
  • 7. SIDE EFFECTS OF HCQ • Nausea , abdominal cramps , diarrhoea • Reduced appetite • Acne , anemia , skin rash • Loss of hair • Vertigo , convulsions • Eye pigmentation • Retinopathy (most dangerous side effect, can cause permanent vision loss)
  • 8. OVERDOSE • Effects shows within an hour of ingestion • Sleepiness • Permanent vision loss • Seizure • Hypotension • Ventricular fibrillation • Respiratory failure
  • 9. CONTRAINDICATION • Patient on anti arrhythmic medication because HCQ can prolong QT interval] • Psoriasis • Porphyria • Renal failure • Lactating mother (HCQ can enter breast milk) • children
  • 10. DRUG INTERACTION • 1. [HCQ & Penicillamine]- increase plasma concentration of penicillamine, which may leads to severe side effects. 2. [HCQ & insulin]- enhances hypoglysemic effcts of insulin 3. [HCQ & antacids]- antacids may decrease the absorption of HCQ.
  • 11. DRUG INTERACTIONS 4. [HCQ & neostigmine/pyridostigmine]- antagonize the action of HCQ. 5. [HCQ & digoxin]- increases serum digoxin levels 6. [HCQ & anti epileptics]- impaie the antiepileptic activity
  • 12. THANKS FOR WATCHING LIKE, COMMENT, SHARE & SUBSCRIBE