Minocycline for Acne

Medical uses

Minocycline is a broad-spectrum tetracycline antibiotic. Minocycline is used to treat a wide variety of bacterial infections, such as dermatologic diseases, urinary tract infections, acne, rosacea, and tick fever.

Most common minocycline side effects are headache, fatigue, dizziness, nausea, vomiting, skin rashes, pruritus13.

Minocycline Efficacy for Acne

Minocyclineis very effective in reducing moderate to moderately-severe inflammatory acne vulgaris. It is even useful in inhibiting granuloma formation. However, currently minocycline is no longer considered the first choice in the treatment of acne, particularly given its potential to cause serious adverse effects8.

Minocycline is highly lipophilic and has an excellent activity in the pilosebaceous complex. This antibiotic has been used in the treatment of moderate to severe papulo-pustular acne for a long time. Minocycline is widely used in persons with acne who fail to respond to other treatments.

Most strains of P. acnes are sensitive to minocycline. The percentage of P. acnes resistant strains is still less than 5%1. It is very important because of increasing rate of P. acnes resistance to other tetracyclines.

Efficacy: Minocycline treatment reduces acne lesion count by about 56-66%10, 12. The clinical success rate (more than 2/3 decrease in inflammatory lesions) is about 64%11.

Dosage for Acne: Minocycline should be started at 100 mg twice daily, but clearing may be maintained at doses as low as 100 mg every 2-3 days.

Benefits

• Great lipophilicity results in excellent sebum penetration and pilosebaceous duct concentration.
• Less phototoxic than other tetracyclines. Studies indicate that photosensitivity occurs rarely with minocycline hydrochloride4.
• Less likelihood of bacterial resistance. Bacterial cell membranes are surrounded by a lipid layer (a water insoluble, fatty substance which surrounds the cell and provides it with fuel). As a means of resisting antibiotics, the cells increase the thickness of this lipid layer. Minocycline has the best penetrating ability5.
• Great tissue penetration. Minocycline penetrates into most body tissues achieves very high tissue concentrations. Equivalent blood and tissue levels achieved whether administered intravenously or orally. Also, minocycline has ability to cross the blood-brain barrier.
• The long half-life allows for a less frequent dosing regimen.
• Minocycline is one of the few drugs that are highly active against methicillin-resistant Staphylococcus aureus (MRSA).
• Minocycline can be taken with food. It causes less gastrointestinal upset than other tetracyclines.

Concerns

• Expensive. Minocycline is quite expensive.
• Intracranial hypertension. Benign intracranial hypertension has been documented in association with minocycline6. Benign intracranial hypertension (BIH) is a rare but potentially serious condition. Benign intracranial hypertension, also known as pseudotumour cerebri, involves a persistent rise in cerebrospinal fluid pressure. It is characterised by headache, nausea, vomiting and papilloedema with occasional sixth-nerve palsy.
• Serious hypersensitivity reactions. Minocycline can cause serum sickness like reaction (SSLR).
• Lupus-like syndrome. Minocycline may produce a lupus-like syndrome. Also rarely, long-term treatment may engender a lupus- like syndrome that is antinuclear-antibody positive and that clears upon discontinuation of the drug. The risk of autoimmune reactions increases with duration of treatment.
• Vestibular dysfunction. Minocycline is associated with a high rate of vestibular side effects, such as dizziness, nausea, vomiting, vertigo, and anorexia 7. This is caused by vestibular or CNS toxicity and is of such severity and frequency that CDC has changed recommendations on its non-essential use.
• Hyperpigmentation.3 Minocycline seems to be unique within the tetracyclines class in causing potentially irreversible slate-grey hyperpigmentation of the skin.

Pharmacological characteristics

• Elimination half-life: 16 hours (range: 11-23 hours)
• Metabolism: minocycline is metabolized in the liver and principally excreted in the biliary tract.
• Excretion: excreted via the faeces primarily and via the urine at a low rate.

Mechanism of action

Minocycline is a tetracycline with antibacterial activity against some Gram-negative and Gram-positive organisms. The action is primarily bacteriostatic and it is thought to exert its antimicrobial effect by the inhibition of protein synthesis.

Neuroprotective effects
Minocycline is thought to inhibit cell death in the central nervous system by reducing the activity of proapoptotic and proinflammatory enzymes. The drug has been shown to be neuroprotective in animal models of stroke, trauma and a variety of neurodegenerative diseases.

Minocycline Alternatives

Alternative oral antibiotics for acne treatment:

• Doxycycline
• Tertacycline

Reviews, Discussions, Forums

• Minocycline ratings, comments by patients on DrugLib.com
• Minocycline user reviews at Drugs.com (user's rating for acne - 7.2 points)

References

• 1. Maffeis L, Veraldi S. Minocycline (Minocin) in the treatment of acne: latest findings. G Ital Dermatol Venereol. 2010 Jun;145(3):425-9.
• 2. Ochsendorf F. Minocycline in acne vulgaris: benefits and risks. Am J Clin Dermatol. 2010;11(5):327-41. PubMed
• 3. Goulden V, Glass D, Cunliffe WJ. Safety of long-term high-dose minocycline in the treatment of acne. Br J Dermatol. 1996 Apr;134(4):693-5. PubMed
• 4. Glette J, Sandberg S. Phototoxicity of tetracyclines as related to singlet oxygen production and uptake by polymorphonuclear leukocytes. Biochem Pharmacol. 1986 Sep 1;35(17):2883-5. PubMed
• 5. Eady EA, Cove JH, Holland KT, Cunliffe WJ. Superior antibacterial action and reduced incidence of bacterial resistance in minocycline compared to tetracycline-treated acne patients. Br J Dermatol. 1990 Feb;122(2):233-44. PubMed
• 6. Lander CM. Minocycline-induced benign intracranial hypertension. Clin Exp Neurol. 1989;26:161-7. PubMed
• 7. Jacobson JA, Daniel B. Vestibular reactions associated with minocycline. Antimicrob Agents Chemother. 1975 Oct;8(4):453-6. PubMedCentral
• 8. Garner SE, Eady A, Bennett C, Newton JN, Thomas K, Popescu CM. Minocycline for acne vulgaris: efficacy and safety. Cochrane Database Syst Rev. 2012 Aug PubMed
• 9. Shi W, Chen Z, Chen X, Cao L, Liu P, Sun S. The combination of minocycline and fluconazole causes synergistic growth inhibition against Candida albicans: an in vitro interaction of antifungal and antibacterial agents. FEMS Yeast Res. 2010 Nov. PubMed
• 10. Bossuyt L, Bosschaert J, Richert B, et al. Lymecycline in the treatment of acne: an efficacious, safe and cost-effective alternative to minocycline. Eur J Dermatol. 2003 Mar-Apr;13(2):130-5.
• 11. Dreno B, Moyse D, Alirezai M, et al. Multicenter randomized comparative double-blind controlled clinical trial of the safety and efficacy of zinc gluconate versus minocycline hydrochloride in the treatment of inflammatory acne vulgaris. Dermatology. 2001;203(2):135-40. PubMed
• 12. Leyden J, Thiboutot DM, Shalita AR, et al. Comparison of tazarotene and minocycline maintenance therapies in acne vulgaris: a multicenter, double-blind, randomized, parallel-group study. Arch Dermatol. 2006 May;142(5):605-12. PubMed
• 13. Solodyn (minocycline hydrochloride) Label PDF

By HealthyStock Research Group, October 2009
Medical resources reviewed: August 2018