Date of approval.
Date of revision.
Alprazolam Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician
Strictly prohibited for food and feed processing
Drug Name
Generic name: Alprazolam Tablets
English name: Alprazolam Tablets
Hanyu Pinyin：Apuzuolun Pian
Ingredients】The main ingredient of this product is: Alprazolam.
Chemical name: 1-methyl-6-phenyl-8-chloro-4H-(1,2,4-triazole)and[4,3-a][1,4]-benzodiazepine.
Chemical structure formula.
Molecular formula: C17H13ClN4
Molecular weight: 308.77
【Properties】.
This product is a white or off-white tablet with indentations on one side.
Indications】
It is mainly used for anxiety, nervousness and agitation, also can be used as an adjunct to hypnosis or anxiety, also as an anti-panic drug, and can relieve acute alcohol withdrawal symptoms. It should be used with caution in patients with mental depression.
Specification】 0.4mg
Dosage
Adult dosage: Anti-anxiety, start with 0.4mg (1 tablet) once, 3 times a day, and increase the dosage as needed. The maximum limit can be 4mg (10 tablets) a day. Sedation and hypnosis: 0.4~0.8mg (1~2 tablets), taken at bedtime. Anti-panic: 0.4mg (1 tablet) 3 times a day, dosage to be increased as needed, up to a maximum of 10mg (25 tablets) a day. for children under 18 years of age, dosage has not been determined.
Adverse reactions
①Common adverse reactions: drowsiness, dizziness, weakness, etc. Ataxia, tremor, urinary retention, jaundice are occasionally seen in high doses. ②Rarely, there are rash, photosensitivity, leukopenia. ③Individual patients experience excitement, polyphonia, sleep disturbance, and even hallucinations. The above symptoms disappear quickly after stopping the drug. ④There is addiction and withdrawal symptoms may occur after long-term application and discontinuation of the drug, manifested as agitation or depression. ⑤A few patients have dry mouth, mental inattention, excessive sweating, palpitations, constipation or diarrhea, blurred vision, and hypotension.
(1) Serious adverse reactions
(1) Dependence (frequency uncertain), withdrawal symptoms (frequency uncertain)
Drug dependence may occur after continuous large doses, and adequate observation is required, and caution should be exercised for overdosing. If the dosage is suddenly reduced or discontinued after taking a large amount of the drug continuously, withdrawal symptoms such as cramps, dizziness, tremors, insomnia, restlessness, hallucinations, and delusions may occur. Therefore, if you need to stop taking the drug, please reduce the dosage gradually and proceed with caution.
(2) Stimulation excitement (frequency uncertain), confusion (frequency uncertain)
Patients with psychiatric disorders such as syndromic disorder may experience reverse stimulation and confusion, so it is necessary to observe them adequately, discontinue them promptly when they occur, and handle them appropriately.
(3) Suppression of breathing (frequency uncertain)
Patients suffering from chronic bronchitis and other respiratory-related diseases may experience inhibition of breathing when taking it, and need to be fully observed, discontinued promptly when abnormalities occur, and handled appropriately.
4) Allergic reactions (frequency uncertain)
When itching, urticaria, flushing, swelling, shortness of breath and other related symptoms occur, discontinue taking it promptly and deal with it appropriately.
(5) Liver function impairment (frequency uncertain), jaundice (frequency uncertain)
The rise of AST (GOT), ALT (GPT), and γ-GTP is likely to be accompanied by liver function impairment. jaundice, the patient’s symptoms need to be adequately observed, discontinued promptly in the event of abnormalities, and properly managed.
(2) Other adverse reactions
Less than 0.1-5% Less than 0.1% Frequency uncertain Mental nervous system Drowsiness, vertigo, dizziness, headache Liver AST (GOT), ALT (GPT), rise in γ-GTP Rise in γ-GTP Circulatory system Palpitations Blood pressure drop Digestive system Thirst, nausea, vomiting, constipation, abdominal pain, abdominal discomfort, loss of appetite Diarrhea **Allergic symptoms Note Rash, pruritus to light Allergic reaction to light Skeletal muscle weakness, tiredness Muscle relaxation and other symptoms of decreased muscle tension Other Sweating
Note: When the above symptoms occur, stop taking it immediately.
Contraindications】① acute alcoholism in which the central nervous system is depressed; ② myasthenia gravis (because of the effect of muscle retardation, there is a possibility of worsening symptoms); ③ acute or easy to occur closed-angle glaucoma attack (because of the anticholinergic effect of this drug increases intraocular pressure, there is a possibility of worsening glaucoma symptoms); ④ severe chronic obstructive pulmonary disease; ⑤ drivers, high-altitude workers, dangerous fine work (6) Patients with a past history of hypersensitivity to this drug; (7) Patients taking the following drugs: HIV protease inhibitors (indinavir, etc.) (see [Drug Interactions] for details).
Precautions] 1. Use with caution (the following patients should be used with caution)
(1) patients with heart disease (may aggravate symptoms); (2) patients with hepatic dysfunction (may prolong the clearance half-life of this drug for metabolic reasons); (3) patients with renal dysfunction (may delay excretion); (4) patients with organic brain disease (drug effect may be enhanced); (5) children, etc. (please refer to [Pediatric Use]); (6) elderly (please refer to [Geriatric Use]); (7) more frail patients (prone to adverse reactions); ⑧ patients with moderate respiratory impairment or severe respiratory impairment (respiratory insufficiency) (possible worsening of symptoms).
Important basic precautions.
①Patients who are allergic to benzodiazepines may be allergic to this drug; ②Sudden discontinuation of the drug in patients with epilepsy may lead to seizures; ③Severe mental depression may aggravate the condition and even produce suicidal tendencies, and precautions should be taken; ④Continuous administration of the drug may lead to dependence, and addiction by continuous long-term heavy dosing should be avoided. Based on the treatment requirements, when long-term continuous use is required, it must be fully discussed (refer to [Adverse Reactions]). If long-term use requires discontinuation of the drug, it is not advisable to stop abruptly, but to gradually reduce the dosage; ⑤ The occurrence of respiratory depression or hypotension often indicates an overdose; ⑥ Patients with low tolerance to this drug should start with a small dosage and gradually increase the dosage; ⑦ After taking this drug, it may cause drowsiness, concentration, concentration, low motor function, etc. Patients taking this drug should be careful not to operate equipment that can cause danger, such as driving, working at height, or delicate work.
Pregnant women and nursing mothers
(1) In the third trimester of pregnancy, this drug may increase the risk of fetal teratogenicity; (2) Long-term use in pregnant women may cause dependence, causing withdrawal symptoms in newborns, and the use of the drug in the second trimester of pregnancy may affect the central nervous activity of newborns, and the use of the drug before and during delivery may result in weaker muscle tone in newborns, so pregnant women should avoid using the drug as much as possible, and should only use the drug if they judge that the therapeutic benefits exceed the risks; (3) This drug can be secreted into breast milk (3) This drug can be secreted into breast milk, and should be used with caution by breastfeeding women.
Children under 18 years old, the dosage has not been specified.
For the elderly
This drug is more sensitive to the elderly, start with a small dose, 0.2mg (0.5 tablets) once, 3 times a day, gradually increase to the maximum tolerable amount, be careful to take (prone to adverse reactions such as motor dysfunction).
Drug Interactions]
(1) Combination with central depressants may increase respiratory depression; (2) Combination with addictive and other potentially addictive drugs increases the risk of addiction; (3) Combination with alcohol and general anesthetics, colistin, analgesics, phenothiazines, monoamine oxidase type A inhibitors and tricyclic antidepressants may increase each other’s effectiveness and the dosage should be adjusted; (4) Combination with antihypertensives and diuretics may increase the hypotensive effect; (5) Combination with cimetidine and propranolol may increase the hypotensive effect. (5) When combined with cimetidine and propranolol, the clearance of this drug is slowed down and the plasma half-life is prolonged; (6) When combined with paromidone, the metabolism of the latter is slowed down and the dosage of paromidone should be adjusted; (7) When combined with levodopa, the efficacy of the latter can be reduced; (8) When combined with rifampin, the elimination of this drug is increased and the blood concentration is reduced; (9) Isoniazid inhibits the elimination of this drug and increases the blood concentration; (10) When combined with digoxin, the blood concentration of digoxin can be increased and the toxicity is caused. (1) Contraindications for concomitant use
(1) Contraindications for simultaneous administration (cannot be taken at the same time)
Drug name clinical symptoms, treatment mechanism, risk element※
HIV protease inhibitor
Indinavir sulfate may cause excessive sedation and inhibit competitive inhibition of respiratory cytochrome P450 will greatly increase the level of the drug in the blood Concurrent administration Note (matters requiring attention when taking concurrently)
Drug name clinical symptoms, treatment mechanism, risk elements ※Neurocentral depressants
Phenothiazine inducers
Barbiturate inducer, etc.
Monoamine oxidase inhibitors increase drowsiness and reduce attention, concentration, and motor function, and may mutually reinforce the inhibitory effect on the central nervous system* Alcohol
（The AUC, clearance half-life, and half-life of ritonavir will become 2.5 times, 0.41 times, and 2.2 times, respectively, and will enhance the inhibitory effect on the central nervous system. The AUC, clearance half-life, and half-life of itaconazole will become 2.8 times, 0.41 times, and 2.7 times, respectively, and will enhance the inhibitory effect on the central nervous system. The maximum concentration, clearance half-life, and half-life of cimetidine in blood will become 1.9 times, 0.58 times, and 1.2 times, respectively. When reducing the dosage of this drug, or when using other anti-ulcer drugs, it is important to consider that the metabolism of this drug in the liver may be hindered* Promethazine
Desipramine may increase the concentration of promethazine and desipramine in the blood to 1.2-1.3 times. Consider that this drug may hinder the metabolism of promethazine and desipramine in the liver. It is possible that the concentration of digoxin in the blood may increase. The mechanism is not clear, especially in the elderly* The metabolism of this drug is mainly related to cytochrome P450 3A, a hepatic metabolizing enzyme.
Drug overdose]
Persistent confusion, severe drowsiness, impaired motor coordination, decreased reflexes, tremors, slurred speech, stumbling, abnormally slowed heartbeat, shortness of breath or difficulty, and severe weakness. Early symptomatic treatment is recommended for overdose or poisoning, monitoring respiration, pulse and blood pressure, gastric lavage and fluids can be administered, and the trachea should be ensured to be open. This includes emetic or gastric lavage and respiratory and circulatory support therapy. Barbiturates should not be used in cases of abnormal excitation. Flumazenil, a benzodiazepine receptor antagonist, can be used for the relief and diagnosis of overdose. Before taking flumazenil (which antagonizes endogenous benzodiazepine-induced neuroleptics), please read the precautions for flumazenil use (contraindications, caution, interactions, etc.).
Pharmacology and Toxicology
This product is a benzodiazepine hypnotic sedative and anxiolytic. The drug acts on benzodiazepine receptors (BZR) in the central nervous system to enhance the binding of the central inhibitory neurotransmitter γ-aminobutyric acid (GABA) to GABAA receptors, promote the opening of chloride channels, hyperpolarize cells, enhance synaptic inhibition mediated by GABAergic neurons, and reduce the excitability of neurons. BZ receptors are divided into type I and type II, and it is believed that type I receptor excitation can explain the anxiolytic effect of BZ drugs. BZ receptors are divided into type I and type II. It is believed that type I receptor excitation can explain the anxiolytic effect of BZ drugs, while type II receptors are associated with the sedative and skeletal muscle relaxation effects of this class of drugs. It can cause inhibition in different parts of the central nervous system, and with increasing dosage, clinical manifestations can range from mild sedation to hypnosis or even coma. It can pass through the placenta and can be secreted into breast milk. It is addictive and can cause allergy in a few patients.
Pharmacokinetics]
Fast and complete absorption by oral administration, plasma protein binding rate is about 80%. The blood concentration peaks 1~2 hours after oral administration, and the blood concentration reaches steady state in 2~3 days; T1/2 is generally 12~15 hours, 19 hours in the elderly. It is metabolized by the liver and the metabolite α-hydroxyaprazolam, which also has some pharmacological activity. It is excreted via the kidney. The accumulation in the body is very small, and the clearance is fast after discontinuation.
Storage
Store under shade and seal.
Package】 PA/Al/PVC composite hard tablets and pharmaceutical aluminum foil package, 10 tablets/plate/box, 10 tablets/plate×2 plate/box, 10 tablets/plate×10 plate/box; 20 tablets/plate/box, 20 tablets/plate×2 plate/box, 20 tablets/plate×5 plate/box.
Execution Standard
【Approval number】.
State Drug Certificate H37021444
Valid period】 24 months.
[Drug marketing license holder
Company name: Shandong Xinyi Pharmaceutical Co.
Registered address: No. 1 Xingping Road, Pingping County
Manufacturer
Company Name: Shandong Xinyi Pharmaceutical Co.
Production Address: No.1 Xingping Road, Pingping County
Postal code: 253100
Contact：0534-2160269
Fax
Fax: 0534-2160268
Web
Address: www.sd-sinepharm.com