Dimedrol-Darnitsa
Dimedrol-Darnitsa Uses, Dosage, Side Effects, Food Interaction and all others data.
Dimedrol-Darnitsa is an antihistamine with anticholinergic and sedative effects. It competes with histamine for H1-receptor sites on effector cells in the GI tract, blood vessels and respiratory tract.
Dimedrol-Darnitsa has anti-histaminic (H1-receptor), anti-emetic, anti-vertigo and sedative and hypnotic properties . The anti-histamine action occurs by blocking the spasmogenic and congestive effects of histamine by competing with histamine for H1 receptor sites on effector cells, preventing but not reversing responses mediated by histamine alone . Such receptor sites may be found in the gut, uterus, large blood vessels, bronchial muscles, and elsewhere . Anti-emetic action is by inhibition at the medullary chemoreceptor trigger zone . Anti-vertigo action is by a central antimuscarinic effect on the vestibular apparatus and the integrative vomiting center and medullary chemoreceptor trigger zone of the midbrain .
Trade Name | Dimedrol-Darnitsa |
Availability | Rx and/or OTC |
Generic | Diphenhydramine |
Diphenhydramine Other Names | Difenhidramina, Diphenhydramine, Diphenhydraminum |
Related Drugs | Gocovri, prednisone, ibuprofen, acetaminophen, hydroxyzine, amitriptyline, lorazepam, ondansetron, cetirizine, loratadine |
Type | |
Formula | C17H21NO |
Weight | Average: 255.3547 Monoisotopic: 255.162314299 |
Protein binding | Some prescribing information records the protein binding of diphenhydramine as approximately 78% while others have suggested the medication is about 80 to 85% bound to plasma proteins. |
Groups | Approved, Investigational |
Therapeutic Class | Sedating Anti-histamine |
Manufacturer | |
Available Country | Georgia |
Last Updated: | September 19, 2023 at 7:00 am |
![Dimedrol-Darnitsa Dimedrol-Darnitsa](https://www.medicinesfaq.com/media/png/dimedrol-darnitsa.png)
Uses
Dimedrol-Darnitsa is used for the treatment of followings:
- Seasonal, perennial, vasomotor rhinitis
- Urticaria, angioneurotic oedema, anaphylaxis
- Pruiritic conditions
- Premedication for emesis and motion sickness
- Miscellaneous like meniere's disease and parkinsonism
Dimedrol-Darnitsa is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Allergic cough, Allergies, Anaphylaxis, Angioedema, Common Cold, Common Cold/Flu, Conjunctival irritation, Cough, Cough Variant Asthma, Cough caused by Common Cold, Eye allergy, Fever, Insect Bites, Insect Stings, Insomnia, Irritative cough, Itching of the nose, Itching of the throat, Motion Sickness, Nasal Congestion, Oral Mucositis, Pain, Parkinsonian Syndromes, Pollen Allergy, Productive cough, Pruritus, Rash, Rhinorrhoea, Sinus Congestion, Sinus headache, Skin Irritation, Sneezing, Sunburn, Symptoms of Acute Bronchitis Accompanied by Coughing, Upper respiratory tract hypersensitivity reaction, site unspecified, Urticaria, Dermatographism, Dry cough, Watery itchy eyes, Airway secretion clearance therapy, Expectorant
How Dimedrol-Darnitsa works
Dimedrol-Darnitsa predominantly works via the antagonism of H1 (Histamine 1) receptors . Such H1 receptors are located on respiratory smooth muscles, vascular endothelial cells, the gastrointestinal tract (GIT), cardiac tissue, immune cells, the uterus, and the central nervous system (CNS) neurons . When the H1 receptor is stimulated in these tissues it produces a variety of actions including increased vascular permeability, promotion of vasodilation causing flushing, decreased atrioventricular (AV) node conduction time, stimulation of sensory nerves of airways producing coughing, smooth muscle contraction of bronchi and the GIT, and eosinophilic chemotaxis that promotes the allergic immune response .
Ultimately, diphenhydramine functions as an inverse agonist at H1 receptors, and subsequently reverses effects of histamine on capillaries, reducing allergic reaction symptoms . Moreover, since diphenhydramine is a first-generation antihistamine, it readily crosses the blood-brain barrier and inversely agonizes the H1 CNS receptors, resulting in drowsiness, and suppressing the medullary cough center .
Furthermore, H1 receptors are similar to muscarinic receptors . Consequently, diphenhydramine also acts as an antimuscarinic . It does so by behaving as a competitive antagonist of muscarinic acetylcholine receptors, resulting in its use as an antiparkinson medication .
Lastly, diphenhydramine has also demonstrated activity as an intracellular sodium channel blocker, resulting in possible local anesthetic properties .
Dosage
Dimedrol-Darnitsa dosage
Adult-
- Most allergic conditions: 25-50 mg three times a day with a further 50 mg at night.
Children-
- 1 to 5 years of age: 5 mg i.e., 2.5 ml of elixir 4 times a day
- More than 6 years of age: 10 mg i.e. 5 ml of elixir 4 times a day
Side Effects
Side effect includes sedation, dizziness, tinnitus, fatigue, ataxia, blurred vision, diplopia, euphoria, and epigastric discomfort.
Toxicity
Overdose is expected to result in effects similar to the adverse effects that are ordinarily associated with the use of diphenhydramine, including drowsiness, hyperpyrexia, and anticholinergic effects, among others . Additional symptoms during overdose may include mydriasis, fever, flushing, agitation, tremor, dystonic reactions, hallucinations and ECG changes . Large overdose may cause rhabdomyolysis, convulsions, delirium, toxic psychosis, arrhythmias, coma and cardiovascular collapse . Moreover, with higher doses, and particularly in children, symptoms of CNS excitation including hallucinations and convulsions may appear; with massive doses, coma or cardiovascular collapse may follow .
Although diphenhydramine has been in widespread use for many years without ill consequence, it is known to cross the placenta and has been detected in breast milk . This medication should therefore only be used when the potential benefit of treatment to the mother exceeds any possible hazards to the developing fetus or suckling infant .
Pharmacokinetic studies indicate no major differences in the distribution or elimination of diphenhydramine compared to younger adults . Nevertheless, diphenhydramine should be used with caution in the elderly, who are more likely to experience adverse effects . Avoid use in elderly patients with confusion .
The results of a review on the use of diphenhydramine in renal failure suggest that in moderate to severe renal failure, the dose interval should be extended by a period dependent on Glomerular filtration rate (GFR) .
After intravenous administration of 0.8 mg/kg diphenhydramine, a prolonged half-life was noted in patients with chronic liver disease which correlated with the severity of the disease . However, the mean plasma clearance and apparent volume of distribution were not significantly affected .
LD50=500 mg/kg (orally in rats). Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death.
Precaution
Caution should be exercised with patients in whom drowsiness is undesirable e.g., drivers, machine operators. Concomitant consumption of alcohol or central nervous system (CNS) depressants will potentiate drowsiness.
Interaction
Dimedrol-Darnitsa administration significantly reduces the absorption of the antituberculous agent para-aminosalicyclic acid (PAS) from the gastrointestinal tract. CNS depressants may potentiate the sedative action of Dimedrol-Darnitsa. Anticholinergic drugs may potentiate Dimedrol-Darnitsa’s anticholinergic side effects.
Food Interaction
- Avoid alcohol.
- Take before a meal. Take 30 minutes before a meal or 30 minutes before departure for motion sickness.
Dimedrol-Darnitsa Alcohol interaction
[Moderate] GENERALLY AVOID:
Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.
In addition, the potential for abuse may be increased with the combination.
The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.
No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.
However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.
Alcohol should generally be avoided during therapy with anticholinergic agents.
Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.
Dimedrol-Darnitsa Drug Interaction
Moderate: duloxetine, duloxetine, pregabalin, pregabalin, alprazolam, alprazolam, cetirizine, cetirizineUnknown: aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Dimedrol-Darnitsa Disease Interaction
Major: depressionModerate: anticholinergic effects, asthma/COPD, cardiovascular, renal/liver disease, glaucoma, liver disease, resp depression
Volume of Distribution
Dimedrol-Darnitsa is widely distributed throughout the body, including the CNS . Following a 50 mg oral dose of diphenhydramine, the volume of distribution is in the range of 3.3 - 6.8 l/kg .
Elimination Route
Dimedrol-Darnitsa is quickly absorbed after oral administration with maximum activity occurring in approximately one hour . The oral bioavailability of diphenhydramine has been documented in the range of 40% to 60%, and peak plasma concentration occurs about 2 to 3 hours after administration .
Half Life
The elimination half-life ranges from 2.4-9.3 hours in healthy adults . The terminal elimination half-life is prolonged in liver cirrhosis .
Clearance
Values for plasma clearance of a 50 mg oral dose of diphenhydramine has been documented as lying in the range of 600-1300 ml/min .
Elimination Route
The metabolites of diphenhydramine are conjugated with glycine and glutamine and excreted in urine . Only about 1% of a single dose is excreted unchanged in urine . The medication is ultimately eliminated by the kidneys slowly, mainly as inactive metabolites .
Pregnancy & Breastfeeding use
Category B: There are no adequate and well controlled studies in pregnant women using diphenhydramine hydrochloride. Therefore, diphenhydramine hydrochloride should be used in pregnancy only if clearly needed. Dimedrol-Darnitsa hydrochloride has been reported to be excreted in breast milk and thus, use of diphenhydramine hydrochloride in lactating mother is not recommended.
Contraindication
Known hypersensitivity to Dimedrol-Darnitsa Hydrochloride, Ammonium chloride is contra-indicated in presence of impaired hepatic or renal function.
Acute Overdose
Symptoms: Impaired consciousness; psychosis, seizures, antimuscarinic symptoms (e.g. mydriasis, tachycardia, tachyarrhythmias), resp failure, rhabdomyolysis; acute delirium with visual and auditory hallucination (topical).
Management: Supportive and symptomatic treatment. Convulsions and marked CNS stimulation may be treated with IV diazepam.
Storage Condition
Store between 15-30° C. Protect from moisture.
Innovators Monograph
You find simplified version here Dimedrol-Darnitsa
Dimedrol-Darnitsa contains Diphenhydramine see full prescribing information from innovator Dimedrol-Darnitsa Monograph, Dimedrol-Darnitsa MSDS, Dimedrol-Darnitsa FDA label
FAQ
What is Dimedrol-Darnitsa used for?
Dimedrol-Darnitsa is an antihistamine used to relieve symptoms of allergy, hay fever, and the common cold. These symptoms include rash, itching, watery eyes, itchy eyes/nose/throat, cough, runny nose, and sneezing. It is also used to prevent and treat nausea, vomiting and dizziness caused by motion sickness.
How safe is Dimedrol-Darnitsa?
The U.S. Food and Drug Administration is warning that taking higher than recommended doses of the common over-the-counter (OTC) allergy medicine diphenhydramine can lead to serious heart problems, seizures, coma, or even death.
How does Dimedrol-Darnitsa work?
Dimedrol-Darnitsa works by blocking the action of histamine, a substance in the body that causes allergic symptoms.
What are the common side effects of Dimedrol-Darnitsa?
Common side effects of Dimedrol-Darnitsa are include:
- dry mouth, nose, and throat
- drowsiness
- dizziness
- nausea
- vomiting
- loss of appetite
- constipation
- increased chest congestion
- headache
- muscle weakness
- excitement (especially in children)
- nervousness
Is Dimedrol-Darnitsa safe during pregnancy?
Dimedrol-Darnitsa is considered to be safe during pregnancy. Doctors and nurses recommend this OTC medication to help relieve allergy symptoms, even while you're pregnant. Recent studies have found Dimedrol-Darnitsa to be safe.
Is Dimedrol-Darnitsa safe during breastfeeding?
Small, occasional doses of Dimedrol-Darnitsa would not be expected to cause any adverse effects in breastfed infants.
Can I drink alcohol with Dimedrol-Darnitsa?
Alcohol may increase drowsiness and dizziness while you are taking Dimedrol-Darnitsa. You should be warned not to exceed recommended dosages and to avoid activities requiring mental alertness. If your doctor prescribes these medications together, you may need a dose adjustment to safely take this combination.
Can I drive after taking Dimedrol-Darnitsa?
Do not drive or operate machinery if Dimedrol-Darnitsa makes you drowsy or affects your judgment.
When should be taken of Dimedrol-Darnitsa?
When Dimedrol-Darnitsa is used to treat motion sickness, it is usually taken 30 minutes before departure and, if needed, before meals and at bedtime.
How often can I take Dimedrol-Darnitsa?
Dimedrol-Darnitsa is usually taken every 4 to 6 hours.
How much Dimedrol-Darnitsa can I take in a day?
For adults and teens, the Dimedrol-Darnitsa dosage is 25 to 50 mg every 4 to 6 hours. The maximum amount you should take in one day is 300 mg. Keep in mind, taking higher doses can increase the risk of side effects, including drowsiness.
Is Dimedrol-Darnitsa bad for my liver?
Despite widespread use over many decades, Dimedrol-Darnitsa has not been linked to liver test abnormalities or to clinically apparent liver injury. The reason for its safety may relate its short half-life and limited duration of use.
How long does Dimedrol-Darnitsa take to work?
It normally takes about 30 minutes to work. Common side effects include feeling sleepy, dizzy or unsteady on your feet. You may also have difficulty concentrating and have a dry mouth.
Can I take Dimedrol-Darnitsa on an empty stomach?
Dimedrol-Darnitsa may be taken with or without food. Take exactly as directed. Do not take more than is recommended.
How long does Dimedrol-Darnitsa stay in my system?
A half-life of a drug determines how long it will take for 50% of it to flush out of your system. Depending on the median value that the individual lands on, Dimedrol-Darnitsa can stay in your system anywhere between 13.2 and 49 hours.
Can Dimedrol-Darnitsa be taken long-term?
Caution should be exercised for long-term use of Dimedrol-Darnitsa, an antihistamine and a non-benzodiazepine sedative-hypnotic, because of the association of increased risk for dementia.
How long can I use Dimedrol-Darnitsa?
Do not use Dimedrol-Darnitsa for longer than 2 weeks to treat sleep problems, or longer than 7 days to treat cold or allergy symptoms.
Who should not take Dimedrol-Darnitsa?
If you have increased pressure in the eye, closed angle glaucoma, high blood pressure, stenosing peptic ulcer you should not take Dimedrol-Darnitsa.
What happen If I suddenly stop taking Dimedrol-Darnitsa?
Although withdrawal symptoms of Dimedrol-Darnitsa are minor compared to harder drugs, you may experience cold sweats, nausea, or diarrhea when stopping the drug suddenly.
What happen If I missed Dimedrol-Darnitsa?
Since Dimedrol-Darnitsa is used when needed, you may not be on a dosing schedule. If you are on a schedule, use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.
What happen if I take too much Dimedrol-Darnitsa?
Taking more than the normal Dimedrol-Darnitsa dosage can be harmful. Serious side effects from too much of the Dimedrol-Darnitsa can include nausea, vomiting, blurred vision, trouble breathing, hallucinations, unconsciousness, and seizures.
Can Dimedrol-Darnitsa cause heart problems?
Taking too much Dimedrol-Darnitsa can lead to serious heart problems, seizures, coma, or death.
Can Dimedrol-Darnitsa cause heart palpitations?
A fast heartbeat is a common side effect of Dimedrol-Darnitsa. In rare cases, it can become serious.
Can Dimedrol-Darnitsa damage kidneys?
In general, Dimedrol-Darnitsa do not cause kidney problems.