Histaverin
Histaverin Uses, Dosage, Side Effects, Food Interaction and all others data.
The relief of pain (analgesia) is a primary goal for enhancing the quality of life of patients and for increasing the ability of patients to engage in day to day activities. Histaverin, an opioid analgesic, was originally approved in the US in 1950 and is a drug used to decrease pain by increasing the threshold for pain without impairing consciousness or altering other sensory functions. Opiates such as codeine are derived from the poppy plant, Papaver somniferum (Papaveraceae).
Histaverin is utilized as a central analgesic, sedative, hypnotic, antinociceptive, and antiperistaltic agent, and is also recommended in certain diseases with incessant coughing.
General effects
Trade Name | Histaverin |
Availability | Prescription only |
Generic | Codeine |
Codeine Other Names | Codein, Codeína, Codéine, Codeine polistirex, Codeinum, Methylmorphine |
Related Drugs | Buprenex, aspirin, acetaminophen, tramadol, naproxen, Tylenol, oxycodone, diphenhydramine, Benadryl, benzonatate |
Type | |
Formula | C18H21NO3 |
Weight | Average: 299.3642 Monoisotopic: 299.152143543 |
Protein binding | 7-25% bound to plasma proteins . |
Groups | Approved, Illicit |
Therapeutic Class | |
Manufacturer | |
Available Country | Spain |
Last Updated: | September 19, 2023 at 7:00 am |
![Histaverin Histaverin](https://www.medicinesfaq.com/media/png/histaverin.png)
Uses
Histaverin is an opioid analgesic used to treat moderate to severe pain when the use of an opioid is indicated.
Histaverin sulfate is a form of this drug that is commonly used. It is available in tablet form and indicated for the relief of mild to moderately severe pain, where the use of an opioid analgesic is appropriate .
The solution form is used by itself or combined in a syrup with other drugs and is used as a cough suppressant in adults aged 18 and above , .
Histaverin is also used to associated treatment for these conditions: Common Cold, Cough, Flu caused by Influenza, Mild pain, Pain, Severe Pain, Dry cough, Moderate Pain, Upper respiratory symptoms, Airway secretion clearance therapy
How Histaverin works
Histaverin is a selective agonist for the mu opioid receptor, but with a much weaker affinity to this receptor than morphine, a more potent opioid drug. Histaverin binds to mu-opioid receptors, which are involved in the transmission of pain throughout the body and central nervous system , . The analgesic properties of codeine are thought to arise from its conversion to Morphine, although the exact mechanism of analgesic action is unknown at this time , .
Toxicity
Oral LD50: 427 mg kg-1 (rat) .
Overdose/toxicity
Symptoms of opioid toxicity may include confusion, somnolence, shallow breathing, constricted pupils, nausea, vomiting, constipation and a lack of appetite. In severe cases, symptoms of circulatory and respiratory depression may ensue, which may be life-threatening or fatal , .
Teratogenic effects
This drug is classified as a pregnancy Category C drug. There are no adequate and well-controlled studies completed in pregnant women. Histaverin should only be used during pregnancy if the potential benefit outweighs the potential risk of the drug to the fetus .
Histaverin has shown embryolethal and fetotoxic effects in the hamster, rat as well as mouse models at about 2-4 times the maximum recommended human dose . Maternally toxic doses that were about 7 times the maximum recommended human dose of 360 mg/day, were associated with evidence of bone resorption and incomplete bone ossification. Histaverin did not demonstrate evidence of embrytoxicity or fetotoxicity in the rabbit model at doses up to 2 times the maximum recommended human dose of 360 mg/day based on a body surface area comparison .
Nonteratogenic effects
Neonatal codeine withdrawal has been observed in infants born to addicted and non-addicted mothers who ingested codeine-containing medications in the days before delivery. Common symptoms of narcotic withdrawal include irritability, excessive crying, tremors, hyperreflexia, seizures, fever, vomiting, diarrhea, and poor feeding. These signs may be observed shortly following birth and may require specific treatment .
Histaverin (30 mg/kg) given subcutaneously to pregnant rats during gestation and for 25 days after delivery increased the rate of neonatal mortality at birth. The dose given was 0.8 times the maximum recommended human dose of 360 mg/day .
The use in breastfeeding/nursing
Histaverin is secreted into human milk. The maternal use of codeine can potentially lead to serious adverse reactions, including death, in nursing infants .
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
Histaverin Alcohol interaction
[Moderate] GENERALLY AVOID:
Ethanol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics.
Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.
In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.
Concomitant use of opioid analgesics with ethanol should be avoided.
Histaverin Drug Interaction
Major: pregabalin, pregabalin, quetiapine, quetiapine, diazepam, diazepam, alprazolam, alprazolamModerate: contained in alcoholic beverages , contained in alcoholic beverages Unknown: acetaminophen, acetaminophen, acetaminophen, acetaminophen, albuterol, albuterol, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Histaverin Disease Interaction
Major: impaired GI motility, infectious diarrhea, liver disease, prematurity, acute alcohol intoxication, drug dependence, gastrointestinal obstruction, hypotension, intracranial pressure, respiratory depressionModerate: adrenal insufficiency, biliary spasm, hypothyroidism, renal dysfunction, seizure disorders, urinary retention, arrhythmias
Volume of Distribution
Apparent volume of distribution: about 3-6 L/kg, showing an extensive distribution of the drug into tissues .
Elimination Route
Absorption
Histaverin is absorbed from the gastrointestinal tract. The maximum plasma concentration occurs 60 minutes after administration .
Food Effects
When 60 mg codeine sulfate was given 30 minutes post-ingestion of a high high-calorie meal, there was no significant change in the absorption of codeine .
Steady-state concentration
The administration of 15 mg codeine sulfate every 4 hours for 5 days lead to steady-state concentrations of codeine, morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) within 48 hours .
Half Life
Plasma half-lives of codeine and its metabolites have been reported to be approximately 3 hours .
Clearance
Renal clearance of codeine was 183 +/- 59 ml min-1 in a clinical study .
Renal impairment may decrease codeine clearance .
Elimination Route
About 90% of the total dose of codeine is excreted by the kidneys. Approximately 10% of the drug excreted by the kidneys is unchanged codeine .
The majority of the excretion products can be found in the urine within 6 hours of ingestion, and 40-60 % of the codeine is excreted free or conjugated, approximately 5 to 15 percent as free and conjugated morphine, and approximately 10-20% free and conjugated norcodeine .
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