Methyldopa injection nonclinical toxicology: Difference between revisions
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==NONCLINICAL TOXICOLOGY== | |||
===Carcinogenesis, Mutagenesis, Impairment of Fertility=== | |||
No evidence of a tumorigenic effect was seen when methyldopa was given for two years to mice at doses up to 1800 mg/kg/day or to rats at doses up to 240 mg/kg/day (30 and 4 times the maximum recommended human dose in mice and rats, respectively, when compared on the basis of body weight; 2.5 and 0.6 times the maximum recommended human dose in mice and rats, respectively, when compared on the basis of body surface area; calculations assume a patient weight of 50 kg). | |||
Methyldopa was not mutagenic in the Ames Test and did not increase chromosomal aberration or sister chromatic exchanges in Chinese hamster ovary cells. These in vitro studies were carried out both with and without exogenous metabolic activation. | |||
Fertility was unaffected when methyldopa was given to male and female rats at 100 mg/kg/day (1.7 times the maximum daily human dose when compared on the basis of body weight; 0.2 times the maximum daily human dose when compared on the basis of body surface area). Methyldopa decreased sperm count, sperm motility, the number of late spermatids and the male fertility index when given to male rats at 200 and 400 mg/kg/day (3.3 and 6.7 times the maximum daily human dose when compared on the basis of body weight; 0.5 and 1 times the maximum daily human dose when compared on the basis of body surface area). | |||
Long-term studies in animals have not been performed to evaluate the carcinogenic potential of methyldopate hydrochloride; nor have evaluations of this ester's mutagenic potential or potential to affect fertility been carried out.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = METHYLDOPATE HYDROCHLORIDE INJECTION, SOLUTION [AMERICAN REGENT, INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=f5f25053-a9f3-48b9-a412-078f5ee942fd | publisher = | date = | accessdate = 10 March 2014 }}</ref> | |||
<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = METHYLDOPATE HYDROCHLORIDE INJECTION, SOLUTION [AMERICAN REGENT, INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=f5f25053-a9f3-48b9-a412-078f5ee942fd | publisher = | date = | accessdate = 10 March 2014 }}</ref> | |||
Revision as of 16:55, 10 March 2014
| Methyldopa |
|---|
| Methyldopa tablet® FDA Package Insert |
| Indications and Usage |
| Dosage and Administration |
| Contraindications |
| Warnings |
| Precautions |
| Adverse Reactions |
| Drug Interactions |
| Use in Specific Populations |
| Overdosage |
| Description |
| Clinical Pharmacology |
| Nonclinical Toxicology |
| How Supplied/Storage and Handling |
| Labels and Packages |
| Methyldopa injection® FDA Package Insert |
| Indications and Usage |
| Dosage and Administration |
| Contraindications |
| Warnings |
| Precautions |
| Adverse Reactions |
| Drug Interactions |
| Use in Specific Populations |
| Overdosage |
| Description |
| Clinical Pharmacology |
| Nonclinical Toxicology |
| How Supplied/Storage and Handling |
| Labels and Packages |
| Clinical Trials on Methyldopa |
| ClinicalTrials.gov |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Abdurahman Khalil, M.D. [2]
NONCLINICAL TOXICOLOGY
Carcinogenesis, Mutagenesis, Impairment of Fertility
No evidence of a tumorigenic effect was seen when methyldopa was given for two years to mice at doses up to 1800 mg/kg/day or to rats at doses up to 240 mg/kg/day (30 and 4 times the maximum recommended human dose in mice and rats, respectively, when compared on the basis of body weight; 2.5 and 0.6 times the maximum recommended human dose in mice and rats, respectively, when compared on the basis of body surface area; calculations assume a patient weight of 50 kg).
Methyldopa was not mutagenic in the Ames Test and did not increase chromosomal aberration or sister chromatic exchanges in Chinese hamster ovary cells. These in vitro studies were carried out both with and without exogenous metabolic activation.
Fertility was unaffected when methyldopa was given to male and female rats at 100 mg/kg/day (1.7 times the maximum daily human dose when compared on the basis of body weight; 0.2 times the maximum daily human dose when compared on the basis of body surface area). Methyldopa decreased sperm count, sperm motility, the number of late spermatids and the male fertility index when given to male rats at 200 and 400 mg/kg/day (3.3 and 6.7 times the maximum daily human dose when compared on the basis of body weight; 0.5 and 1 times the maximum daily human dose when compared on the basis of body surface area).
Long-term studies in animals have not been performed to evaluate the carcinogenic potential of methyldopate hydrochloride; nor have evaluations of this ester's mutagenic potential or potential to affect fertility been carried out.[1]
References
- ↑ "METHYLDOPATE HYDROCHLORIDE INJECTION, SOLUTION [AMERICAN REGENT, INC.]". Retrieved 10 March 2014.