hydroxychloroquine

1. HYDROXY-CHLOROQUINE
[HCQ]
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

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