Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Traditional IUPAC Name
pKa (strongest acidic)
pKa (Strongest Basic)
Dược Lực Học :
Desmopressin is a synthetic analogue of the natural antidiuretic hormone (ADH or vasopressin) that is produced by the hypothalamus and stored in the posterior pituitary gland. The main function of ADH is to regulate extracellular fluid volume in the body. ADH secretion is stimulated by angiotensin II, linking it to the renin-angiotensin-aldosterone system (RAAS). ADH stimulates water reabsorption in the kidneys by causing the insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. It also causes vasoconstriction through its action on vascular smooth muscle cells of the collecting tubules. The efficacy of desmopressin for managing bleeds in patients with hemophilia A or von Willebrand’s disease Type I arises from its ability to elicit dose-dependent increases in plasma factor VIII (antihemophilic factor), plasminogen activator, and to a lesser extent, factor VIII-related antigen and ristocetin cofactor activities; these changes improve blood clotting.
Cơ Chế Tác Dụng :
Desmopressin is a chemical that is similar to Antidiuretic Hormone (ADH) which is found naturally in the body. It increases urine concentration and decreases urine production. Desmopressin is used to prevent and control excessive thirst, urination, and dehydration caused by injury, surgery, and certain medical conditions, allowing you to sleep through the night without awakening to urinate. It is also used to treat specific types of diabetes insipidus and conditions after head injury or pituitary surgery.
Desmopressin emulates the actions of endogenous human ADH (refer to Pharmacology section above). Desmpressin is a structural analogue of ADH modified by deamination of 1-cysteine and substitution of 8-L-arginine by 8-D-arginine. Compared to natural ADH, desmopressin elicits a great antidiuretic response on weight basis.
Dược Động Học :
▧ Absorption :
Minimally absorbed from the GI tract (average absolute bioavailability = 0.08-0.16%). 10-20% absorbed from nasal mucosa.
▧ Protein binding :
▧ Metabolism :
Metabolic fate unknown. Is not affected by liver microsomal cytochrome P450 enzymes.
▧ Half Life :
Oral t1/2=1.5-2.5 hours. Intranasal t1/2=3.3-3.5 hours. IV t1/2 is biphasic: initial t1/2=7.8 minutes, terminal t1/2=0.4-4 hours.
Độc Tính :
Overdose may lead to increased duration of action and lead to symptoms such as fluid retention, headaches, abdominal cramps, nausea, and facial flushing. Adverse effects include headache, nausea, abdominal pain, facial flushing, dizziness, dry mouth, and hyponatremia. Nasal congestion and rhinitis have been reported with nasal spray formulations.
Chỉ Định :
Oral formulations may be used to manage primary nocturnal enuresis in adults and vasopressin sensitive diabetes insipidus, and for control of temporary polyuria and polydipsia following head trauma or surgery in the pituitary region. Intranasal and parenteral formulations may be used to manage spontaneous or trauma-induced bleeds (e.g. hemarthrosis, intramuscular hematoma, mucosal bleeding) in patients with hemophilia A or von Willebrand's disease Type I. May also be used parenterally to prevent or treat bleeding in patients with uremia.
Tương Tác Thuốc :
Opioids may enhance the adverse effects and toxicity of desmopressin. It is recommended to monitor therapy.
Liều Lượng & Cách Dùng :
Liquid - Intravenous - 15 mcg/ml
Liquid - Parenteral - 4 mcg/ml
Spray - Nasal - 0.1 mg/ml
Spray, metered - Nasal - 0.1 mg/ml; 10 mcg per spray
Spray, metered - Nasal - 1.5 mg/ml; 100 mcg per activation
Tablet - Oral - 0.1 mg
Tablet - Oral - 0.2 mg
Tablet, orally disintegrating - Sublingual - 120 mcg
Tablet, orally disintegrating - Sublingual - 240 mcg
Tablet, orally disintegrating - Sublingual - 60 mcg
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Tài Liệu Tham Khảo Thêm
National Drug Code Directory