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Promethazine hydrochloride 58-33-3 Promethazine
Molecular Formula | C17H21ClN2S |
Molar Mass | 320.88 |
Melting Point | 230-232°C |
Boling Point | 403.7 °C at 760 mmHg |
Flash Point | 9℃ |
Solubility | Easily soluble in water, soluble in ethanol or chloroform, almost insoluble in acetone or ether |
Appearance | White or off-white powder |
Color | White to Almost white |
Maximum wavelength(λmax) | ['297nm(H2O)(lit.)'] |
Merck | 14,7786 |
BRN | 4166397 |
PH | pH (50g/L, 25℃) : 4.0~6.0 |
Storage Condition | 2-8°C |
Sensitive | Sensitive to light |
MDL | MFCD00012652 |
Use | Applicable to various allergic diseases and pregnancy Vomit |
Overview | promethazine hydrochloride, also known as Phenergan, is a commonly used clinical phenothiazine antihistamine, although clinical reports of its adverse reactions are not uncommon, but because of its clear role, low price, is still widely used in primary hospitals. Promethazine hydrochloride is the first found phenothiazine-like structure of tricyclic antihistamines, antitussive efficacy, able to competitively block the histamine H1 receptor and produce antihistamine effect, against histamine-induced telangiectasia, and reduce its permeability. As a result, Cough of those caused by tracheal irritation can be relieved. |
pharmacokinetics | absorption is fast and complete and protein binding is high after oral or injection administration. This product by oral or rectal administration after the onset time is 20 minutes, the general duration of antihistamine effect is 6-12 hours, the sedative effect can last for 2-8 hours. Mainly in the liver metabolism, inactive metabolites can be excreted by urine, fecal excretion of less. |
pharmacological action | promethazine is an antihistamine of the phenothiazine class, and can also be used for antiemetic, anti-halo, and sedative-hypnotic. 1. Antihistamine effect: it competes with histamine released from tissues for H1 receptor, and can antagonize the contraction or contracture of smooth muscle of gastrointestinal tract, trachea, bronchi or bronchioles by histamine, relieves the spasmogenic and hyperemic effect of histamine on bronchial smooth muscle. 2. Antiemetic effect: it may be related to the inhibition of emetic chemical sensing area of medulla oblongata. 3. Anti-motion sickness: it may act on the vestibular and Vomit Central and midbrain medullary receptors through central anticholinergic properties, mainly blocking the excitation of Cholinergic Synaptic labyrinth Impulse in the vestibular nucleus. 4, sedative hypnotic effect: may be due to indirectly reduce the brain stem network up the activation system of the stress. |
indication | 1. Skin and mucous membrane allergy: for long-term, seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis caused by contact with allergens or food, urticaria, angioedema, allergic reactions to blood or plasma products, scarification of skin. If necessary, it can be combined with epinephrine as an adjuvant of the drug. Motion sickness: prevention and treatment of motion sickness, seasickness and aircraft sickness. 3. Sedation and hypnosis: Applicable to preoperative, postoperative and obstetric. In addition, it can also be used to reduce the fear of adults and children, in a light sleep state. Nausea, Vomit treatment: suitable for some anesthesia and surgery Nausea, Vomit, also for the prevention and treatment of radiation disease or drug-induced Nausea, Vomit. 5. Postoperative pain: it can be combined with pain medication as an adjuvant. |
usage and dosage | . 2. The dosage should be reduced at the time of dehydration or Oliguria to avoid toxic reaction. 3. When oral, can be taken with food or milk at the same time, in order to reduce the stimulation of gastric mucosa. 4. Adult usual dosage: Oral: ① anti-allergy, 12.5mg(0.5 tablets), 4 times a day, after meals and before going to bed, 25mg(1 tablet) before going to bed if necessary; ② antiemetic, at the beginning, 25mg(1 tablet) once, 12.5~25mg(0.5 ~ tablets) every 4~6 hours if necessary; ③ anti-vertigo, 25mg(1 tablet) once, sedation and hypnosis, 25~50mg(1~2 tablets), if necessary, double. 5. Children's usual dosage: Oral: ① anti-allergy, each time according to the weight of 0.125mg/kg or according to the body surface area of 3.75mg/m2, once every 4~6 hours, or according to the weight of 0.25~0.5mg/kg or according to the body surface area of 7.5~15mg/m2 before going to bed; According to The Age, the daily amount of 5~10mg within 1 year old, 1~5 years old 5~15mg,6 years old over 10~25mg, can be given once or twice, according to the body weight of 0.25 ~ 0.5mg/kg or according to the body surface area of 7.5 ~ 15mg/m2; If necessary, every 4~6 hours administration; ③ Anti vertigo, 0.25~0.5mg/kg of body weight or 7.5~15mg/m2 of body surface area; If necessary, every 12 hours, or 12.5~25mg, 2 times a day; ④ sedation and hypnosis, if necessary, 0.5 to 1 mg/kg of body weight or 15 to 30mg/m2 of body surface area. |
adverse reactions | promethazine belongs to phenothiazine derivatives, with no obvious side effects in small doses, however, the common side effects of thiazide can occur in large and long-term use. 1. Increase the sensitivity of the skin to light, more nightmares, easily excited, easily excited, hallucinations, toxic delirium, children prone to extrapyramidal reactions. The above reaction rate was not high. 2. Signs and symptoms of excessive dosage include: clumsiness or erratic movements of hands and feet, drowsiness or flushing in severe cases, Fever, shortness of breath or Dyspnea, increased heart rate [antimuscarinic (M) receptor effect], muscle cramps, especially in the neck and back muscles. Restlessness, difficulty walking, spasmodic twitching of the muscles of the head and face or tremor of the hands (the latter is extrapyramidal effect). 3. Care should be taken when the following conditions persist: somnolence is more common; Blurred vision or color blindness (mild) is less common; Dizziness, dry mouth and nasopharynx, tinnitus, rash, stomach pain or stomach discomfort, unresponsiveness (more common in children), Nausea or Vomit [with surgery and/or other drugs], and even jaundice. Rectal burning or tingling may occur when using suppositories. 4. Cardiovascular adverse reactions are rare, with increased blood pressure and occasional mild decrease in blood pressure. Leukopenia, granulocytopenia, and regenerating anemia are rare. |
note | 1. Skin allergy. Known to be highly allergic to phenothiazine drug patients, also allergic to this product. 2. Interference with diagnosis: increased glucose tolerance can be shown in glucose tolerance test. Can interfere with the urine pregnancy immune test, the results were false positive or false negative. 3. The following should be used with caution: acute asthma, bladder neck obstruction, myelosuppression, cardiovascular disease, Coma, angle-closure glaucoma, hepatic insufficiency, hypertension, gastric ulcer, prostatic hypertrophy, pyloric or Duodenal obstruction, respiratory diseases (especially in children, after taking this product sputum viscous, affecting expectoration, and can inhibit Cough reflex), epilepsy patients (injection administration can increase the severity of convulsions), jaundice, various liver diseases and renal failure, Reye syndrome (extrapyramidal symptoms due to promethazine are easily confused with Reye syndrome). 4. When using promethazine, special attention should be paid to whether there is intestinal obstruction, or drug overdose, poisoning and other problems, because its symptoms and signs can be covered by promethazine's antiemetic effect. |
Use | applies to a variety of allergic diseases and pregnancy Vomit. indications: it can competitively block the Hl receptor of the group limbs to produce antihistamine effect, antagonize histamine-induced telangiectasia, reduce its permeability, and relieve wheezing caused by bronchial smooth muscle contraction, compared with diphenhydramine hydrochloride, the effect was strong and lasting. |
CAS:
58-33-3
MF:
C17H21ClN2S
MW:
320.88
EINECS:
200-375-2
MDL No.:
MFCD00012652
Melting point:
230-232°C
Flash point:
9℃
storage temp.
2-8°C
solubility
Very soluble in water, freely soluble in ethanol (96 per cent) and in methylene chloride.
color
White to Almost white
PH
pH (50g/L, 25℃) : 4.0~6.0
λmax
297nm(H2O)(lit.)
Merck
14,7786
BRN
4166397
BCS Class
1,3
InChI
InChI=1S/C17H20N2S.ClH/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H
InChIKey
XXPDBLUZJRXNNZ-UHFFFAOYSA-N
SMILES
N1(CC(C)N(C)C)C2C=CC=CC=2SC2=CC=CC=C12.Cl
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