Oxetamol
Oxetamol Uses, Dosage, Side Effects, Food Interaction and all others data.
Oxazepam is a short-acting benzodiazepine. It increases neuronal membrane permeability to Cl ions by binding to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron w/in the CNS (including the limbic system, reticular formation) and enhancing the GABA inhibitory effects resulting in hyperpolarisation and stabilisation.
Benzodiazepines, including oxazepam, exert their sedative and anxiolytic effects by potentiating the effects of endogenous GABA, the primary inhibitory neurotransmitter in the CNS. Compared to other benzodiazepines, it has relatively low potency and a moderate duration of action. Oxazepam should be administered with caution to patients for whom a drop in blood pressure may lead to cardiac complications as, in rare cases, it may cause hypotension.
Paracetamol exhibits analgesic action by peripheral blockage of pain impulse generation. It produces antipyresis by inhibiting the hypothalamic heat-regulating centre. Its weak anti-inflammatory activity is related to inhibition of prostaglandin synthesis in the CNS.
Paracetamol (Acetaminophen) is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat dissipation.
| Trade Name | Oxetamol |
| Generic | Oxazepam + Paracetamol |
| Weight | 250mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Islamabad Pharmaceutical Products |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Oxazepam is used in the treatment of anxiety disorders, including anxiety associated with depression. This drug seems to be particularly effective for anxiety, tension, agitation and irritability in older people. It is also prescribed to relieve symptoms of acute alcohol withdrawal.
Paracetamol IV is used for the management of mild to moderate pain, the management of moderate to severe pain with adjunctive opioid analgesics, the reduction of fever.
Paracetamol is a non-salicylate antipyretic and non-opioid analgesic agent. Paracetamol IV injection is a sterile, clear, colorless, non pyrogenic, isotonic formulation of Paracetamol intended for intravenous infusion.
Oxetamol is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Anxiety DisordersAcute Gouty Arthritis, Acute Musculoskeletal Pain, Allergies, Ankylosing Spondylitis (AS), Arthritis, Chills, Cold, Cold Symptoms, Common Cold, Common Cold/Flu, Cough, Cough caused by Common Cold, Coughing caused by Flu caused by Influenza, Dyskinesia of the Biliary Tract, Dyskinesia of the Urinary Tract, Febrile Convulsions, Febrile Illness Acute, Fever, Fibromyalgia Syndrome, Flu caused by Influenza, Headache, Joint dislocations, Menstrual Distress (Dysmenorrhea), Mild pain, Muscle Inflammation, Muscle Injuries, Muscle Spasms, Musculoskeletal Pain, Nasal Congestion, Neuralgia, Osteoarthritis (OA), Pain, Pollen Allergy, Postoperative pain, Premenstrual cramps, Rheumatoid Arthritis, Rhinopharyngitis, Rhinorrhoea, Severe Pain, Sinusitis, Soreness, Muscle, Spasms, Spastic Pain of the Gastrointestinal Tract, Sprains, Tension Headache, Toothache, Upper Respiratory Tract Infection, Whiplash Syndrome, Acute Torticollis, Mild to moderate pain, Minor aches and pains, Minor pain, Moderate Pain, Airway secretion clearance therapy, Antispasmodic, Bronchodilation
How Oxetamol works
Like other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy.
Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha (α) and gamma (γ) subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased.
Dosage
Oxetamol dosage
Adult:
- Mild to Moderate Anxiety with Tension, Irritability and Agitation: The usual dose is 10 to 15 mg 3 or 4 times per day.
- Severe Anxiety, Depression with Anxiety, or Alcohol Withdrawal: The usual dose is 15 to 30 mg, 3 or 4 times per day.
Children: Safety and effectiveness have not been established for children less than 6 years of age, nor have dosage guidelines been established for children 6 to 12 years. Doctor will adjust the dosage to fit the child's needs.
Older adults: The usual starting dose is 10 mg, 3 times a day. Doctor may increase the dose to 15 mg 3 or 4 times a day, if needed.
Renal Impairment: No dosage adjustment needed.
Adults and adolescents weighing 50 kg and over: the recommended dosage of Paracetamol IV is 1000 mg every 6 hours or 650 mg every 4 hours, with a maximum single dose of Paracetamol IV of 1000 mg, a minimum dosing interval of 4 hours, and a maximum daily dose of Paracetamol of 4000 mg per day.
Adults and adolescents weighing under 50 kg: the recommended dosage of Paracetamol IV is 15 mg/kg every 6 hours or 12.5 mg/kg every 4 hours, with a maximum single dose of Paracetamol IV of 15 mg/kg, a minimum dosing interval of 4 hours, and a maximum daily dose of Paracetamol of 75 mg/kg per day.
Children >2 to 12 years of age: the recommended dosage of Paracetamol IV is 15 mg/kg every 6 hours or 12.5 mg/kg every 4 hours, with a maximum single dose of Paracetamol IV of 15 mg/kg, a minimum dosing interval of 4 hours, and a maximum daily dose of Paracetamol of 75 mg/kg per day.
Side Effects
Side effects cannot be anticipated. If any develop or change in intensity, doctor should be informed immediately. Doctor will determine if it is safe for a patient to continue taking Oxazepam. More common side effect includes drowsiness. Less common or rare side effects include: Blood disorders, change in libido, dizziness, excitement, fainting, headache, liver problems, loss or lack of muscle control, nausea, skin rashes or eruptions, sluggishness or unresponsiveness, slurred speech, swelling due to fluid retention, tremors, vertigo, yellowed eyes and skin. Side effects due to rapid decrease or abrupt withdrawal from Oxazepam: Abdominal and muscle cramps, convulsions, depressed mood, inability to fall or stay asleep, sweating, tremors, vomiting.
As all paracetamol products, adverse drug reactions are rare (>1/10000, <1/1000) or very rare (<1/10000). Frequent adverse reactions at injection site have been reported during clinical trials (pain and burning sensation). Very rare cases of hypersensitivity reactions ranging from simple skin rash or urticaria to anaphylactic shock have been reported and require discontinuation of treatment. Cases of erythema, flushing, pruritus and tachycardia have been reported.
Toxicity
The oral LD50 in rats and mice is >8000 mg/kg and 1540 mg/kg, respectively.
Symptoms of oxazepam overdose are likely to be consistent with its adverse effect profile and range from mild to severe, sometimes fatal, CNS depression. Treatment should include gastric decontamination, via lavage or induced vomiting, followed by symptomatic and supportive measures. The benzodiazepine antagonist flumazenil may be used in hospitalized patients as an adjunct to non-pharmacological management, but may increase the risk of seizure in long-term benzodiazepine users and in cyclic antidepressant overdose.
Precaution
This drug may make dizzy, drowsy or cause blurred vision; caution should be taken while engaging in activities requiring alertness such as driving or using machinery. Limit should be maintained while taking alcoholic beverages. Caution is advised when using this drug in the elderly because they may be more sensitive to the effects of the drug, especially the drowsiness effect.
Administration of Paracetamol in doses higher than recommended may result in hepatic injury, including the risk of severe hepatotoxicity and death. Do not exceed the maximum recommended daily dose of Paracetamol. Use caution when administering Paracetamol in patients with the following conditions: hepatic impairment or active hepatic disease, alcoholism, chronic malnutrition, severe hypovolemia (e.g., due to dehydration or blood loss), or severe renal impairment (creatinine clearance < 30 ml/min). There were infrequent reports of life-threatening anaphylaxis requiring emergent medical attention. Discontinue Paracetamol IV immediately if symptoms associated with allergy or hypersensitivity occurs. Do not use Paracetamol IV in patients with Paracetamol allergy.
Interaction
Oxazepam may intensify the effects of alcohol. It may be best to avoid alcohol while taking this medication. If Oxazepam is taken with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with a doctor before combining Oxazepam with the following:
- Antihistamines such as Diphenhydramine
- Narcotic painkillers such as Oxycodone and Pethidine
- Sedatives such as Secobarbital and Triazolam
- Tranquilizers such as Diazepam and Alprazolam
Volume of Distribution
Volume of distribution is about 0.9L/kg. 10 to 20% of the drug is bound to red blood cells. Acetaminophen appears to be widely distributed throughout most body tissues except in fat.
Elimination Route
Following oral administration, peak plasma levels (Cmax) averaged 450 mg/mL and occurred approximately 3 hours (Tmax) after dosing.
Half Life
The mean elimination half-life of oxazepam is 8.2 hours.
The half-life for adults is 2.5 h after an intravenous dose of 15 mg/kg. After an overdose, the half-life can range from 4 to 8 hours depending on the severity of injury to the liver, as it heavily metabolizes acetaminophen.
Clearance
Adults: 0.27 L/h/kg following a 15 mg/kg intravenous (IV) dose. Children: 0.34 L/h/kg following a 15 mg/kg intravenous (IV dose).
Elimination Route
Oxazepam is primarily eliminated in the urine as its glucuronide metabolite, with the feces containing approximately 21% of the unchanged drug. The majority of an orally ingested dose of oxazepam is excreted within 48 hours.
Pregnancy & Breastfeeding use
This medication is not recommended for use during pregnancy due to the potential possible fetal harm. Based on information from related drugs, this drug may pass into breast milk and may have undesirable effects on a nursing infant. Therefore, breast-feeding while using this medication is not recommended.
Pregnancy Category C. There are no studies of intravenous Paracetamol in pregnant women; however, epidemiological data on oral Paracetamol use in pregnant women show no increased risk of major congenital malformations. Animal reproduction studies have not been conducted with IV Paracetamol and it is not known whether Paracetamol IV can cause fetal harm when administered to a pregnant woman. Paracetamol IV should be given to a pregnant woman only if clearly needed. There are no adequate and well-controlled studies with Paracetamol IV during labor and delivery; therefore, it should be used in such settings only after a careful benefit-risk assessment. While studies with Paracetamol IV have not been conducted, Paracetamol is secreted in human milk in small quantities after oral administration.
Contraindication
The drug is contraindicated in individuals who have an allergic reaction to Oxazepam or other benzodiazepines such as diazepam. Oxazepam should not be prescribed if any patient is being treated for mental disorders which are more serious than anxiety.
Paracetamol is contraindicated in patients with known hypersensitivity to its active ingredient or to any of the excipients in the intravenous formulation. Also contraindicated in patients with severe hepatic impairment or severe active liver disease
Special Warning
Pediatric Use: The safety and effectiveness of Paracetamol IV for the treatment of acute pain and fever in pediatric patients ages 2 years and older is supported by evidence from adequate and well-controlled studies of Paracetamol IV in adults.
Geriatric use: No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients.
Patients with Hepatic Impairment: Paracetamol is contraindicated in patients with severe hepatic impairment or severe active liver disease and should be used with caution in patients with hepatic impairment or active liver disease. A reduced total daily dose of Paracetamol may be warranted.
Patients with Renal Impairment: In cases of severe renal impairment (creatinine clearance < 30 ml/min), longer dosing intervals and a reduced total daily dose of Paracetamol may be warranted.
Acute Overdose
An overdose of Oxazepam can be fatal. Symptoms of mild Oxazepam overdose may include: Confusion, drowsiness, lethargy. Symptoms of more serious overdose may include: Coma, hypnotic state, lack of coordination, limp muscles and low blood pressure.
Storage Condition
Store in a cool and dry place, protected from light and moisture. Keep out of reach of children.
Store in a cool & dry place & away from children. For single use only. The product should be used within 6 hours after opening. Do not refrigerate or freeze.
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