BioMed Research International / 2014 / Article / Tab 1

Review Article

New Perspectives on Antiacne Plant Drugs: Contribution to Modern Therapeutics

Table 1

An overview of available therapies for acne and associated factors.

ClassDrugDoseMode of actionClinical evidenceAdverse effectsReference

RetinoidsTretinoin0.01–0.05%Anti comedogenic effect, indirect antimicrobiotic effect; anti-inflammatory, ability to regulate keratinocyte desquamationMild comedonal acneLow grade irritant dermatitis with erythema and scaling, burning, photosensitivity[4, 3438, 42]
Isotretinoin1.0–2.0 mg/kg/dayInhibits sebaceous gland differentiation and proliferation, reduces sebaceous gland size, suppresses sebum production, normalizes follicular epithelial desquamation, regulates keratinocyte—keratinocyte adhesion, antiinflammatory effectSevere recalcitrant
nodular acne
Cheilitis, conjunctivitis, hyper triglyceridemia, elevated serum cholesterol levels and liver enzymes, blood dyscrasias, dry eyes and mouth, photosensitivity, and pruritus; incidence/risk of teratogenicity, myalgia, arthralgia, headaches, malaise, mood swings and depression; acne fulminans, characterized by extensive erosive lesions, fever, arthralgias, leukocytosis premature epiphyseal closure in young children, asthma exacerbation, skin fragility, spectrum of ophthalmological disturbances, from dry eyes to optic neuritis
Adapalene0.1%–0.3%Anti comedogenic effect, indirect antimicrobiotic effectMild to moderate
comedonal acne
Irritation, contraindicated in pregnant women
Tazarotene0.05% or 0.1%
Retinol0.04%–0.07%Photosensitivity, xerosis, cheilitis

KeratolyticsAzelaic acid20%Anticomedogenic and antimicrobial effect, reduces the production of keratohyalin granules in the pilosebaceous duct and thus normalizes the ductal hypercornification; keratolytic and anti-inflammatoryMild to moderate acne Only a slight sensation of burning or tingling, mild erythema[3436, 42]
Benzoyl peroxide1%–10%Antimicrobial effect (reactive oxygen species are generated that kill bacteria by oxidizing constituents of their cell membranes), antiinflammatory, very mild anti comedogenic effects, keratolyticInflammatory acne,
Mild to moderate acne
Irritant dermatitis with erythema and scaling, dryness, peeling, stinging, or burning, bleach hair, clothes, and bed linens
Salicylic acid2%Anti-inflammatory, topical desquamating agent, comedolyticComedonal acnePeeling, hyperpigmentation, toxic inner ear damage, hypoglycemia, hypersensitivity, acute salicylate intoxication[36, 37]
Sulfur1–10%Keratolytic activityMalodor and dry skin
Zinc200 mg/day (Zn gluconate), 400 or 600 mg/day (Zn sulfate )Bacteriostatic, inhibits chemotaxis, and may decrease tumor necrosis factor—α productionMild or moderate acne, severe and inflammatory acneNausea, vomiting, and diarrhoea with gastrointestinal side effects
Alpha hydroxyl acids (Glycolic and lactic acid)10%Exfoliative capabilities, promotes epidermolysis, disperse basal layer melanin, increases collagen synthesis within the dermis
Sodium sulfacetamide10% with 5% sulphurInhibiting P. acnes proliferation, act through competitive antagonism of para-aminobenzoic acid, halting bacterial DNA synthesisInflammatory lesions and
comedones
Mild transient dryness, itching

AntibioticsErythromycin2%–4%Antimicrobial effect, a significant decrease of free fatty acids of the skin surface lipids, as a marker of P. acnes lipase activity, indirect anticomedogenic effect, suppress leukocyte chemotaxis and bacterial lipase activityModerate to severe
inflammatory acne
Bacterial resistance and cross resistance[4, 3436, 38, 42]
Clindamycin1%Antibacterial, anti-inflammatoryInflamed lesionsAntibiotic resistance, diarrhoea, pseudomembranous colitis
Tetracycline500 to 1000 mg/daySuppress leukocyte chemotaxis and bacterial lipase activityModerate to severe inflammatory acneDrug-induced lupus erythematous or a dose-duration pigmentation, abdominal colic, diarrhoea and vaginal candidiasis, enamel hypoplasia and a yellowish discoloration of the forming teeth, gastrointestinal discomfort, less commonly, photosensitivity, esophagitis, pancreatitis and pseudo-porphyria
Minocycline75–200 mg/dayInhibits cytokines and matrix metalloproteinases thought to contribute to inflammation and tissue breakdownMild papulopustular acneUrticaria to drug induced lupus, vertigo, dizziness, ataxia, and rarely a bluish discoloration of the skin, autoimmune hepatitis, hyper sensitivity syndrome
Doxycycline50 to 100 mg twice DailyPhotosensitivity reactions, gastrointestinal disturbances
Trimethoprim/
Sulfamethoxazole
Anti-inflammatory effect, antibacterial, blocks dihydrofolate reductase/dihydropteroate synthetase, which ultimately diminishes bacterial purine and pyrimidine synthesisThrombocytopenia, agranulocytosis anemia, hypersensitivity

Hormonal therapySpironolactone50–100 mg/dayAndrogen receptor blocker, which decreases androgen-stimulated sebocyte proliferation, inhibit androgen biosynthesis by decreasing type II 17α-hydroxysteroid dehydrogenase, therefore halting the conversion of androstenedione to testosterone, inhibition of 5 α-reductase and increased steroid-hormone binding globulin together resulting in 30–50% reduction in sebum excretionModerate acne in womenHyperkalemia, diuretic effect, dysmenorrhea, dysphoria, breast tenderness menstrual irregularities, lethargy, headache, lightheadedness, dizziness, orthostatic hypotension, gynaecomastia in men [35, 38, 38, 40]
Flutamide250–500 mg/dayConverted to its highly potent metabolite, 2-hydroflutamide, which acts to selectively inhibit the binding of dihydrotestosterone to the androgen receptorHepatotoxicity and GIT disturbances, hot flashes, and decreased libido
Cyproterone acetate50–100 mg/dayReduce sebum production, comedogenesisHepatotoxicity, breast tenderness, headache, nausea, breakthrough bleeding
Ethinyl estradiol20–35 µgReduce the production of androgens and sebum by inhibiting LH and FSH, thereby suppressing ovulation and ovarian androgen production, increasing sex hormone binding globulin and by decreasing levels of freely circulating testosterone and inhibit ovarian androgen productionNausea, mood changes, contraindications to using OCs in an otherwise healthy woman include smoking, migraine headaches with aura and hypertension
Norgestimate, Norethindrone, Drospirenone35  gSuppress ovarian androgens and reduce bioavailable testosterone by an estrogen-mediated increase in steroid hormone binding globulin
prednisone2.5 to 5 mg/dAdrenal androgen-production blockers

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