Rectal administration of propylthiouracil in hyperthyroid patients: comparison of suspension enema and suppository form. 2002

W Jongjaroenprasert, and W Akarawut, and D Chantasart, and L Chailurkit, and R Rajatanavin
Division of Endocrinology and Metabolism, Department of Medicine, Ramathidodi Hospital, Mahidol University, Bangkok, Thailand.

Previous studies have described the therapeutic effects of propylthiouracil (PTU) and methimazole in normal subjects after rectal suppositories. The goal of our study was to compare the pharmacokinetic and pharmacologic effects of a suppository and suspension form of PTU given per rectum. Fifteen newly diagnosed hyperthyroid patients of both genders (ages 21 to 55 years) were randomly given the drug as follows: group 1 (n = 7), a single enema (400 mg of PTU in 90 mL of sterile water) and group 2 (n = 8), two suppositories of polyethylene glycol base (200 mg of PTU in each). The pharmacokinetic study revealed earlier time to peak levels (T(max)) and significantly greater maximal peak levels (C(max)) in group 1 than in group 2, (85.71 +/- 12.12 minutes vs. 172.5 +/- 26.24 minutes for T(max) and 3.89 +/- 0.34 vs. 2.01 +/- 0.38 microg/mL, p < 0.05 for C(max), respectively). However, the area under the curve (635.16 +/- 105.71 vs. 377.87 +/- 68.09 microg x min/mL) was not statistically different between both groups. Both forms induced a significant decrease in serum free triiodothyronine (FT(3)) levels and an increase in serum rT(3) levels shortly after administration. Four subjects reported a bitter taste 5-10 minutes after receiving the drug. PTU can be effectively absorbed via the rectal route. The enema form appeared to provide better bioavailability than the suppository form. However, both preparations exhibited comparable therapeutic effect.

UI MeSH Term Description Entries
D006980 Hyperthyroidism Hypersecretion of THYROID HORMONES from the THYROID GLAND. Elevated levels of thyroid hormones increase BASAL METABOLIC RATE. Hyperthyroid,Primary Hyperthyroidism,Hyperthyroidism, Primary,Hyperthyroids
D008297 Male Males
D011441 Propylthiouracil A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534) 6-Propyl-2-Thiouracil,6 Propyl 2 Thiouracil
D004733 Enema Insertion of a solution or compound through the RECTUM with the purpose of cleansing the COLON or for diagnostic procedures. Enemata,Enemas,Enematas
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000285 Administration, Rectal The insertion of drugs into the rectum, usually for confused or incompetent patients, like children, infants, and the very old or comatose. Anal Drug Administration,Drug Administration, Rectal,Instillation, Rectal,Rectal Drug Administration,Drug Administration, Anal,Rectal Administration,Administration, Anal Drug,Administration, Rectal Drug,Administrations, Anal Drug,Administrations, Rectal,Administrations, Rectal Drug,Anal Drug Administrations,Drug Administrations, Anal,Drug Administrations, Rectal,Instillations, Rectal,Rectal Administrations,Rectal Drug Administrations,Rectal Instillation,Rectal Instillations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D013488 Suppositories Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature. Rectal Suppositories,Vaginal Suppositories,Vaginal Suppository,Suppositories, Rectal,Suppositories, Vaginal,Suppository, Vaginal
D013974 Thyroxine The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism. L-Thyroxine,Levothyroxine,T4 Thyroid Hormone,3,5,3',5'-Tetraiodothyronine,Berlthyrox,Dexnon,Eferox,Eltroxin,Eltroxine,Euthyrox,Eutirox,L-3,5,3',5'-Tetraiodothyronine,L-Thyrox,L-Thyroxin Henning,L-Thyroxin beta,L-Thyroxine Roche,Levo-T,Levothroid,Levothyroid,Levothyroxin Deladande,Levothyroxin Delalande,Levothyroxine Sodium,Levoxine,Levoxyl,Lévothyrox,Novothyral,Novothyrox,O-(4-Hydroxy-3,5-diiodophenyl) 3,5-diiodo-L-tyrosine,O-(4-Hydroxy-3,5-diiodophenyl)-3,5-diiodotyrosine,Oroxine,Sodium Levothyroxine,Synthroid,Synthrox,Thevier,Thyrax,Thyroxin,Tiroidine,Tiroxina Leo,Unithroid,L Thyrox,L Thyroxin Henning,L Thyroxin beta,L Thyroxine,L Thyroxine Roche,Levo T,Thyroid Hormone, T4

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