Pruritus and Systemic Disease Medication

Updated: Mar 03, 2020
  • Author: David F Butler, MD; Chief Editor: William D James, MD  more...
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Medication

Medication Summary

The goals of pharmacotherapy are to reduce morbidity and prevent complications.

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Detoxifying agents

Class Summary

These agents are used to treat renal pruritus.

Activated charcoal (Charcodote)

Activated charcoal is the drug of choice for the initial treatment of renal pruritus. Its mechanism of action is unknown, but it is thought to bind an unknown pruritogen. Sorbitol and flavoring are added to some forms to enhance palatability.

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Topical agents

Class Summary

Topical agents are used to treat localized renal pruritus.

Capsaicin topical

Capsaicin is derived from plants of the Solanaceae family. It may render skin and joints insensitive to pain and pruritus by depleting substance P in peripheral sensory neurons, decreasing the transmission of sensation. If is for localized pruritus only.

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Immunomodulatory agents

Class Summary

Immunomodulatory agents are used to treat recalcitrant renal or cholestatic pruritus.

Thalidomide (Thalomid)

Thalidomide is thought to decrease T helper cells while inhibiting the production of TNF-alpha, which may induce itching. It has a strong central depressant effect that may decrease pruritus. Because of adverse events, attempt other treatments first.

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Bile Acid Lowering Agents

Class Summary

These agents are used to treat cholestatic pruritus.

Cholestyramine (Prevalite, Questran)

Cholestyramine is an anion-exchange resin that binds bile acids in the GI tract, interrupting their enterohepatic circulation; it is primarily used to lower cholesterol. Patients must have adequate bile flow for the drug to be effective. Consider this therapy early in cases of hepatic cholestasis because it is inexpensive and may provide relief (within 1-3 wk). Pruritus returns within weeks of discontinuation.

Ursodeoxycholic acid/ursodiol (Actigall, Urso 250, Urso Forte)

Ursodeoxycholic acid/ursodiol is a hydrophilic bile acid that alters the hydrophilicity and distribution of total bile acids and increases the excretion of hydrophobic bile acids. It decreases damage to the hepatocyte membrane by decreasing the uptake of hydrophobic bile acids at the terminal ileum (and likely in hepatocytes). Ursodeoxycholic acid/ursodiol is first-line treatment for patients with intrahepatic cholestasis of pregnancy; it normalizes laboratory values and decreases morbidity and mortality to the fetus by reducing exposure to bile acids.

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Hepatic enzyme inducing agents

Class Summary

These agents are used to treat cholestatic pruritus.

Rifampin (Rifadin)

Rifampin is traditionally used as an antibiotic with the known mechanism of action of inhibiting RNA synthesis in bacteria. It also inhibits the reuptake of hepatic bile acid and induces hepatic mixed-function oxidases, which may detoxify hepatic bile acids. Consider this drug when a course of cholestyramine fails.

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Opioid antagonist agents

Class Summary

These agents are used to treat cholestatic pruritus.

Naloxone (Narcan)

Naloxone is an opioid antagonist and is given intravenously; therefore, it should only be used in emergency treatment of exacerbations of cholestatic pruritus in a hospital setting. A low-dose infusion may be used for 24 hours before oral naltrexone or nalmefene to avoid opioid withdrawal syndrome (sometimes seen in patients given oral opioid antagonists).

Naltrexone (ReVia, Vivitrol)

Naltrexone may also be considered if patients with cholestatic pruritus do not respond to cholestyramine and rifampin. Naltrexone can be administered orally and has a longer half-life than naloxone.

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Anti-inflammatory agents

Class Summary

Anti-inflammatory agents are used to treat polycythemia rubra vera.

Aspirin (Anacin, Ascriptin, Bayer Aspirin, Bayer Buffered Aspirin)

Aspirin appears to decrease platelet degranulation of serotonin and prostaglandins, which contribute to pruritus. It is first-line treatment for symptomatic control of pruritus related to polycythemia vera. Relief may last 12-24 hours.

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Antidepressant agents

Class Summary

These drugs are used to treat generalized pruritus in patients with advanced cancer or polycythemia vera.

Mirtazapine (Remeron, Remeron SolTab)

Mirtazapine is a relatively new antidepressant and is not as widely used as sertraline. It exhibits both noradrenergic and serotonergic activity. In cases of depression associated with severe insomnia and anxiety, mirtazapine has been shown to be superior to other SSRI drugs.

Paroxetine (Paxil, Paxil CR)

Paroxetine is a potent selective inhibitor of neuronal serotonin reuptake. Its mechanism of relieving pruritus is unknown. Effects occur within a few days but may last only 4-6 weeks.

Doxepin (Sinequan, Adapin)

Doxepin is a TCA that has potent H1-blocking activity, making it quite useful for urticaria. However, it has very potent sedative and anticholinergic effects. It can be quite effective if used at bedtime because the sedative effects can help a patient with pruritus sleep.

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Analgesic opioid agents

Class Summary

Agents with central analgesic action may be useful. May alter perception and response to varied stimuli.

Butorphanol (Stadol)

Butorphanol is a mixed agonist-antagonist narcotic with central analgesic effects for moderate to severe pain. It causes less smooth muscle spasm and respiratory depression than morphine or meperidine. Weigh the advantages against the increased cost of butorphanol.

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Immunosuppressant agents

Class Summary

These agents may prevent release of inflammatory cytokines from mast cells.

Pimecrolimus (Elidel)

Pimecrolimus is the first nonsteroid cream approved in United States for mild-to-moderate atopic dermatitis. It is derived from ascomycin, a natural substance produced by the fungus Streptomyces hygroscopicus var ascomyceticus. It selectively inhibits the production and release of inflammatory cytokines from activated T cells by binding to the cytosolic immunophilin receptor macrophilin-12. The resulting complex inhibits phosphatase calcineurin, thus blocking T-cell activation and cytokine release. Cutaneous atrophy has not been observed in clinical trials, a potential advantage over topical corticosteroids. Pimecrolimus is indicated only after other treatment options have failed. Use short-term and for intermittent use only.

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