醋酸甲羥孕酮
醋酸甲羥孕酮 (MPA) 是一種強效的合成**孕激素**(黃體素衍生物)。 過去在獸醫學中,它常被用於行為修飾(例如:遊蕩、雄性間的攻擊行為、噴尿)和皮膚疾病(如貓心因性脫毛)。然而,由於其**引發嚴重副作用的風險極高**,目前的使用已大幅減少。 **臨床要點:** 對於行為問題,現在強烈建議使用更安全的替代方案(如 SSRIs、TCAs 或外科結紮)。MPA 偶爾仍用於特定的生殖適應症,例如懷孕母犬的黃體功能不全、良性前列腺肥大的短期管理,或德國牧羊犬的腦下垂體侏儒症。由於其具有深遠的全身性影響,在使用前必須仔細權衡潛在益處與引發內分泌及生殖系統併發症的巨大風險。
作用機制: MPA mimics endogenous progesterone by binding to intracellular **progesterone receptors**, translocating to the nucleus, and altering gene transcription. It transforms the proliferative endometrium into a secretory endometrium and inhibits spontaneous uterine contractions. * **Endocrine/Reproductive:** Exerts negative feedback on the hypothalamus and pituitary, decreasing **GnRH** → suppressing **FSH** and **LH** release, thereby inhibiting estrus and spermatogenesis. It also possesses anti-estrogenic properties and decreases plasma testosterone. * **Glucocorticoid Activity:** MPA has significant intrinsic affinity for **glucocorticoid receptors**, leading to profound suppression of the hypothalamic-pituitary-adrenal (HPA) axis (decreased ACTH and cortisol release). * **Metabolic Effects:** Induces peripheral insulin resistance, which can precipitate **diabetes mellitus**. * **Growth Hormone:** In dogs, progestins can stimulate the mammary glands to produce growth hormone, potentially leading to acromegaly.
各物種劑量
- Behavioral disorders (reduce marking in neutered males) · 5-20 mg/kg SC or IM three to four times yearly · SC/IM · 3-4 times yearly · Use when all other drugs have been unsuccessful.
- Feline psychogenic alopecia and dermatitis · 75-150 mg IM or SC · IM/SC · Repeat as necessary, but never more often than every 2-3 months
- Progestagen-responsive dermatitis · 50-100 mg IM · IM · May repeat in 3-6 months if needed
- Recurrent abortion secondary to progesterone-deficiency · 1-2 mg/kg IM once weekly · IM · q7d · Stop treatment 7-10 days prior to parturition
- Long-term reproductive control · 2.5-5 mg PO once weekly; 25 mg injected every 6 months to postpone estrus · PO/IM/SC · q7d (PO) or q6mo (Injection)
- Long-term reproductive control · 2 mg/kg IM q5 months · IM · q5 months
- Management of spring transition, prevention of estrus behavior, induction of estrous cycle synchrony, pregnancy maintenance, modification of stallion behavior · 500 to 800 mg IM · IM · Interval varies · Most injections last 2 to 3 months · Will not prevent pregnancy loss and does not stop cyclicity.
- Antipruritic and to suppress ovulation · 0.025-1 mL (3 mg/100 grams body weight) IM once every 4-6 weeks · IM · q4-6w · May cause obesity, fatty liver, polydipsia/polyuria and lethargy if used repeatedly.
給藥途徑
禁忌症
- Pre-pubescent cats or dogs
- Diabetes mellitus
- Pseudopregnant bitches
- Females in diestrus or with prolonged heat
- Uterine hemorrhage or discharge
- Pregnancy (unless specifically treating hypoluteoidism)
不良反應
- Increased thirst (polydipsia) and urination (polyuria)
- Increased appetite (polyphagia) and weight gain
- Depression, lethargy, and personality changes
- Adrenocortical depression (HPA axis suppression)
- Mammary changes (enlargement, milk production, neoplasia)
- Diabetes mellitus
- Pyometra / Cystic endometrial hyperplasia
- Temporary inhibition of spermatogenesis
- Permanent local alopecia, skin atrophy, and depigmentation (with SC injection)
- Acromegaly (in dogs)
藥物相互作用
- Aminoglutethimide · May decrease medroxyprogesterone effects
- Felbamate · May increase medroxyprogesterone metabolism
- Rifampin · May decrease progestin activity due to microsomal enzyme induction and increased progestin metabolism
監測
- Weight
- Blood glucose (draw baseline before therapy and monitor periodically)
- Mammary gland development
- Adrenocortical function
- Clinical efficacy
過量
No specific reports on inadvertent acute overdosage were located. Overdose is expected to manifest as an exaggeration of adverse effects, including profound adrenal suppression, lethargy, metabolic derangements (hyperglycemia), and reproductive tract changes. Treatment should be supportive and symptomatic.
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。