Veterinary Drug Handbook (VDH) is the reference veterinarians turn to when they want an independent source of information on the drugs that are used in veterinary medicine today.

QUINACRINE HCL

Chemistry - A synthetic acridine derivative anthelmintic, quinacrine HCl occurs as a bright yellow, odorless, crystalline powder having a bitter taste. It is sparingly soluble in water. Quinacrine HClmay also be known as mepacrine HCl.

Storage, Stability, Compatibility

Tablets should be stored in tight, light-resistant containers atroom temperature. Quinacrine is not stable in solution for any length of time; however, it may becrushed and mixed with foods to mask its very bitter taste.

Pharmacology - QUINACRINE HCL

Quinacrine's mechanism of action for its antiprotozoal activity against Giardia isnot understood, however it does bind to DNA by intercalation to adjacent base pairs, therebyinhibiting RNA transcription and translocation. Additional y, quinacrine interferes with electrontransport, inhibits succinate oxidation and cholinesterase. Quinacrine binds to nucleoproteins which(in humans at least) can suppress lupus erythromatosis (LE) cell factor.
Uses, Indications - While quinacrine has activity against a variety of protozoans and helminths, itsuse against all but Giardia and Trichomonas has been superseded by safer or more effective agents.
In humans, quinacrine may also be used for treatment of mild to moderate discoid lupuserythromatosis, transcervically as a sterilizing agent or in powder form as an intrapleural sclerosingagent.

Pharmacokinetics - QUINACRINE HCL

Quinacrine is absorbed well from the GI tract or after intrapleural administration. It is distributed throughout the body, but CSF levels are only 1-5% of those found in theplasma. Drug is concentrated in the liver, spleen, lungs and adrenals. It is relatively highly bound toplasma proteins in humans (80-90%). Quinacrine crosses the placenta, but only small amountsenter maternal milk.
Quinacrine is eliminated very slowly (half life in humans: 5-14 days). Quinacrine is slowly metabolized, but primarily eliminated by the kidneys. Acidifying the urine will increase renal excretionsomewhat. Significant amounts may be detected in the urine up to 2 months after drug discontinuation.

Contraindications, Precautions, Reproductive Safety

In humans, quinacrine is relatively contraindicated in patients with psychotic disorders, psoriasis, or porphyria as it may exacerbate theseconditions. Veterinary relevance is unknown.
Quinacrine crosses the placenta and has been implicated in causing a case of renal agenesis andhydrocephalus in a human infant. In high doses, it also has caused increased fetal death rates inrats. Weigh the potential benefits with the risks when considering use in pregnant animals.

Adverse Effects, Warnings

In small animals, a yel owing of skin and urine color can occur, butis not of clinical importance (does not indicate jaundice). Additionally, gastrointestinal disturbances(anorexia, nausea, vomiting, diarrhea), abnormal behaviors ("fly biting", agitation), pruritus, andfever have been noted.
Potentially hypersensitivity reactions, hepatopathy, aplastic anemia, corneal edema and retinopathycould occur (all reported rarely in humans, primarily with high dose long term use).

Overdosage, Acute Toxicity

Overdosage may be serious depending on the dose. In humans, adose as low as 6.8 grams (administered intraduodenally) caused death. Symptoms associated withacute toxicity include CNS excitation (including seizures), GI disturbances, vascular collapse andcardiac arrhythmias. Treatment consists of gut emptying protocols, and supportive and symptomatictherapies. Urinary acidification with ammonium chloride and forced diuresis (with adequate fluidtherapy) may be beneficial in enhancing urinary excretion of the drug.

Drug Interactions

Quinacrine increases the toxicity of primaquine (generally not used in veterinary medicine), and the two should not be used simultaneously. Quinacrine may cause a"disulfiram-reaction" if used with alcohol. Quinacrine concentrates in the liver and should beused with caution with hepatoxic drugs (clinical significance unknown).
Laboratory Considerations - When urine is acidic, quinacrine can cause it to turn a deep yellowcolor. By causing an interfering fluorescence, quinacrine can cause falsely elevated values ofplasma and urine cortisol values.
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