Biodramina for Children 12,5 Mg 12 Single Dose Sachets Oral Solution 2,5 Ml

Biodramina for Children 12,5 Mg 12 Single Dose Sachets Oral Solution 2,5 Ml

ACTION AND MECHANISM

- [ANTIALERGIC], [HISTAMINERGIC ANTAGONIST (H-1)]. Dimenhydrinate is an equimolar complex of diphenhydramine and a theophylline derivative, 7-chloro-theophylline. Diphenhydramine is a derivative of ethanolamine, which competitively, reversibly and non-specifically blocks H1 receptors, decreasing the systemic effects of histamine. It leads to vasoconstriction and decreased vascular permeability, reducing redness and edema associated with allergy. Partially mitigates symptoms associated with allergic processes such as eye redness or nasal congestion. It also produces a slight bronchodilator effect and a decrease in skin itching.
Dimenhydrinate is a nonspecific H1 antagonist, which is why it is capable of antagonizing other receptors such as central and peripheral cholinergic receptors. By crossing the blood-brain barrier and blocking H1 and muscarinic receptors, it will cause sedation, but lighter than ethanolamines.
- [MUSCARINIC CHOLINERGIC ANTAGONIST (M)], antiemetic. Dimenhydrinate is a nonspecific antagonist capable of also blocking other receptors such as central or peripheral muscarinic receptors. The blockade of central H1 and cholinergic receptors could have an antiemetic effect, although this is not completely clear. It has been possible to verify that this drug is capable of inhibiting vestibular stimulation, firstly inhibiting the stimuli formed in the otolic system, and at higher doses, in the semicircular canals. Following continued use, a tolerance to the antiemetic effects has been noted.

PHARMACOKINETICS

- Absorption: Dimenhydrinate is well absorbed in the intestine, but undergoes a strong first-pass hepatic effect. After the administration of a dose, the effects appear within 15-30 minutes, and their duration is 3-6 hours. The Tmax is 2 hours.

- Distribution: Dimenhydrinate is widely distributed throughout the body, crossing the blood-brain and placental barriers. It is also excreted in small amounts with milk.

- Metabolism: It is rapidly and almost completely metabolized in the liver.

- Elimination: The metabolites are eliminated in the urine.

INDICATIONS

- Prevention and treatment of [NAUSEA], [VOMITING] and [VERTIGO] associated with [CINETOSIS].

POSOLOGY

- Children 7-12 years: 6-12 ml (24-48 mg). Maximum dose 36 ml (approx. 150 mg)/24 h.
- Children 2-6 years: 3-6 ml (12-24 mg). Maximum dose 18 ml (approx. 75 mg)/24 h.
- Children under 2 years: safety and efficacy have not been evaluated.
Administer at least 30 min before the trip, and preferably 1-2 h before. The dose can be repeated every 6-8 hours during the trip, without exceeding the maximum doses.

RULES FOR CORRECT ADMINISTRATION

Administration with food : administer with food, water or milk to reduce gastric discomfort.

CONTRAINDICATIONS

- Hypersensitivity to any component of the drug. There may be cross-reactions with other antihistamines, so it is not recommended to use any H1 antihistamine in patients who have presented hypersensitivity to any compound of the group.
- [ASTHMATIC CRISIS]. For some authors, dimenhydrinate could worsen asthma, so its use in an acute crisis is not recommended.
- [PORFYRIA]. H1 antihistamines have been associated with the appearance of porphyric outbreaks, so they are not considered safe in these patients.

PRECAUTIONS

- [RENAL INSUFFICIENCY]. Safety and efficacy in patients with renal insufficiency have not been evaluated, but dimenhydrinate metabolites are excreted in the urine, so their accumulation could occur. Since these metabolites could be active, it might be necessary to prolong the administration periods in patients with renal insufficiency, especially in moderate or severe cases (CLcr less than 60 ml/minute).
- [LIVER FAILURE]. Dimenhydrinate is extensively metabolized by hepatic metabolism. In case of hepatic insufficiency, an increase in plasmatic concentration could occur, with the consequent risk of adverse effects. A dose adjustment may be necessary in these patients depending on the degree of liver function.
- Patients suffering from [GLAUCOMA], [PROSTATIC HYPERPLASIA] or [URINARY BLADDER OBSTRUCTION], [ARTERIAL HYPERTENSION], [CARDIAC ARRHYTHMIA], [MIASTENIA GRAVIS], [PEPTIC ULCERA] stenosing or [INTESTINAL OBSTRUCTION]. Due to the anticholinergic effects of dimenhydrinate, a worsening of these pictures could occur, so it is recommended to exercise extreme caution and suspend treatment in the event of a worsening.
- Diseases of the lower respiratory tree, such as [ASTHMA], [PULMONARY EMPHYSEMA] or [CHRONIC OBSTRUCTIVE PULMONARY DISEASE]. According to some authors, H1 antihistamines could decrease the volume of bronchial secretions, increasing their viscosity, due to their anticholinergic effects, and therefore could aggravate these conditions. However, there is not much clinical evidence, despite which, extreme precautions are recommended in these patients. As a general rule, its use is not recommended in patients with asthmatic attacks (See Contraindications).
- [EPILEPSY]. Caution should be exercised in epileptic patients, since antihistamines have occasionally been associated with paradoxical hyperexcitability reactions, even at therapeutic doses, and therefore could lower the seizure threshold.
- [APPENDICITIS]. Due to its antiemetic effects, it could interfere with the diagnosis of appendicitis. It is recommended to previously rule out the presence of appendicitis in patients with vomiting of unknown origin.
- Ototoxicity. Dimenhydrinate can have a beneficial effect in cases of vertigo, tinnitus, and dizziness, so it could mask ototoxicity induced by ototoxic drugs such as parenteral aminoglycosides, carboplatin, cisplatin, chloroquine, and erythromycin, among others.
- Photosensitivity. Dimenhydrinate could give rise to photosensitivity phenomena, so it is recommended not to sunbathe during treatment, and to protect yourself with sunscreens.
- Extreme temperatures. H1-antihistamines may aggravate dehydration-exhaustion syndrome and heat stroke due to decreased sweating caused by their anticholinergic effects. It is recommended that patients being treated with these drugs avoid exposure to very high temperatures, especially in the case of young children, the elderly or people with serious chronic diseases. It is also advisable to follow adequate hygienic-dietary measures, such as adequate aeration and hydration.

PRECAUTIONS RELATED TO EXCIPIENTS

- This medicine contains sucrose. Patients with hereditary [FRUCTOSE INTOLERANCE], glucose-galactose malabsorption, or sucrase-isomaltase insufficiency should not take this medicine.

- This medicine contains amaranth as an excipient. May cause allergic-type reactions including [ASTHMA], especially in patients with [ALLERGY TO SALICYLATES].

- This medicine contains sucrose. Its use in oral liquids and pharmaceutical forms that remain in contact with the mouth for some time can harm the teeth.

ADVICE TO THE PATIENT

- Administer when symptoms appear, along with food to reduce gastric discomfort. In sensitive people, it could be administered 1-2 hours before the trip.
- The administration may be repeated during the trip, as long as the intervals between doses are respected and the maximum recommended dose is not exceeded.
- It can cause drowsiness, so caution is recommended when driving, and do not combine it with drugs or other sedative substances such as alcohol.
- Patients undergoing treatment with sedative drugs are not advised to self-medicate with products containing dimenhydrinate without consulting a doctor.
- It is advisable not to sunbathe during treatment.
- The doctor should be notified of any chronic pathology that the patient presents before starting treatment.
- Exposure to extreme temperatures should be avoided while using this medication, keeping in a cool environment, adequately hydrating.

SPECIAL WARNINGS

- Dimenhydrinate could mask the ototoxic effects of some drugs, so it is recommended to periodically evaluate acoustic functionality in patients treated with these drugs.
- Before using this medication in patients with vomiting of unknown origin, it is recommended to rule out the presence of appendicitis.
- It is recommended to monitor the patient's hydration in the event of a heat wave, and especially if the patient is a small child, an elderly person or a person with a serious illness.
- Due to the antiallergic effects of this medicine, it could give false negatives in skin tests for hypersensitivity to antigenic extracts. It is recommended to suspend the administration of this medicine at least 72 hours before the test.

INTERACTIONS

Dimenhydrinate could mask the symptoms induced by ototoxic drugs by decreasing vertigo or dizziness. Similarly, it could potentiate the photosensitizing effects of other active principles that give rise to photosensitivity reactions. In addition, drug interactions have been described with the following active ingredients:
- Ethyl alcohol. The joint administration of alcohol and dimenhydrinate could potentiate the sedative effects of both substances. It is recommended to avoid alcohol consumption during treatment.
- Anticholinergics (antiparkinsonians, tricyclic antidepressants, MAOIs, neuroleptics). The administration of dimenhydrinate together with other anticholinergic drugs could potentiate the anticholinergic effects, so it is recommended to avoid the association.
- Sedatives (opioid analgesics, barbiturates, benzodiazepines, antipsychotics). The co-administration of dimenhydrinate together with a sedative drug could potentiate the hypnotic action. It is recommended to extreme precautions.

PREGNANCY

FDA category B. In studies carried out in rats and rabbits using doses 20-25 times higher than those in humans, they have not shown harm to the fetus. There have been no adequate and well-controlled studies in humans. However, dimenhydrinate has been used in cases of hyperemesis gravidarum without significant adverse effects. However, there are reports on a possible association between administration during the last two weeks of pregnancy and the appearance of retrolenticular fibroplasia in premature infants. Although the possibility of harming the fetus seems remote, this medicine should only be used when the benefits outweigh the possible risks.

LACTATION

Dimenhydrinate could inhibit lactation due to its anticholinergic effects. It is also excreted in breast milk in small amounts, although it is unknown if these could have effects on the infant. However, children are more sensitive to anticholinergic reactions and may more frequently present paradoxical hyperexcitability reactions. It is recommended to stop breastfeeding or avoid the administration of this medicine.

CHILDREN

The use of dimenhydrinate in children under two years of age, especially neonates and infants, is not recommended because they may be more susceptible to anticholinergic adverse effects. In children older than 2 years, cases of paradoxical reactions with hyperexcitability have been described, especially at high doses, so it is recommended to use it with caution.

SENIORS

The elderly are more sensitive to the adverse effects of antihistamines, such as dizziness, sedation, confusion, hypotension, and hyperexcitability, as well as anticholinergic effects (dry mouth, urinary retention, glaucoma precipitation). Antihistamines can be used in patients older than 65 years, but precautions must be taken. If the side effects persist or are severe, it is advisable to discontinue treatment.

EFFECTS ON DRIVING

Dimenhydrinate may substantially affect the ability to drive and/or operate machinery. Patients should avoid operating dangerous machinery, including automobiles, until they are reasonably certain that drug treatment will not adversely affect them.

ADVERSE REACTIONS

The side effects of dimenhydrinate are usually mild and transient, being more frequent during the first days of treatment. Like other ethanolamines, dimenhydrinate causes mainly drowsiness and anticholinergic phenomena, but there is great interindividual variability with respect to the frequency and intensity of symptoms, affecting mainly young children and the elderly. The most common adverse reactions are:
- Digestive. [NAUSEA], [VOMITING], [CONSTIPATION], [DIARRHEA], [EPIGASTRIC PAIN], [ANOREXIA], [DRY MOUTH]. These symptoms can be lessened by taking the antihistamine with food.
- Neurological/psychological. The appearance of [SLEEPY] is common (1-9%), especially at the beginning of treatment, and it usually subsides after 2-3 days. [HEADACHE], [VERTIGO] and [DIZZINES] have also been described. Exceptionally, cases of paradoxical [EXCITABILITY] have been observed, especially in young children. This hyperexcitability occurs with [INSOMNIA], [NERVOUSNESS], [CONFUSION], [TREMBOR], [IRRITABILITY], [EUPHORIA], [DELUSION], palpitations and even [CONVULSIONS].
- Cardiovascular. On specific occasions, and normally in case of overdose, [TACHYCARDIA], [PALPITATIONS] and other [CARDIAC ARRYTHMIA] such as [EXTRASYSTOLE] or [CARDIAC BLOCK] can occur. These effects could be due to anticholinergic activity. On occasions [HYPOTENSION] or [ARTERIAL HYPERTENSION] have been described.
- Respiratory. Sometimes an increase in the viscosity of bronchial secretions can occur, which can make breathing difficult.
- Genitourinary. [URINARY RETENTION] and [SEXUAL IMPOTENCE] may appear due to cholinergic blockade.
- Hematological. [HEMOLYTIC ANEMIA], [AGRANULOCYTOSIS], [LEUKOPENIA], [THROMBOCYTOPENIA] or [PANCITOPENIA] have been rarely described.
- Eyepieces. Due to the anticholinergic activity, [GLAUCOMA] and [VISION DISORDERS] such as [MIDRIASIS], [BLURRED VISION] or [DIPLOPIA] could occur.
- Allergic/dermatological. [HYPERSENSITIVITY REACTIONS] may appear after the systemic administration of antihistamines, which can even produce [ANAPHYLAXIS]. [PHOTOSENSITIVITY REACTIONS] may also appear after intense exposure to sunlight, with [DERMATITIS], [PRURITUS], [EXANTEMATIC ERUPTIONS] and [ERYTHEMA].

ADVERSE REACTIONS RELATING TO EXCIPIENTS

- Because it contains methyl parahydroxybenzoate, it can cause [ALLERGY TO PARABENS], possibly delayed.

- Because it contains amaranth (E-123) it can cause [HYPERSENSITIVITY REACTIONS].

OVERDOSE

Symptoms: Symptoms usually appear after 2 hours, although they can last for 18 hours, and are usually variable, being more severe in children and people over 65 years of age. Moderate nervous depression, with sedation and apnea, cardiovascular collapse, hyperexcitability with insomnia, hallucinations, tremors or seizures, and anticholinergic symptoms such as dry mouth, blurred vision, and urinary retention have been reported. Fever above 41.8 ºC may also appear.
In the most serious cases, especially in children, the symptoms could worsen, appearing hypotension, convulsions, respiratory depression, loss of consciousness, coma and death.
Treatment: Treatment will consist of the usual measures designed to favor the elimination of the drug. The administration of emetics is usually ineffective. Although a gastric lavage may be beneficial if less than 3 hours have elapsed since ingestion.
The patient will be kept calm to minimize stimulation of the central nervous system. Seizures can be treated with diazepam in adults and phenobarbital in children at a dose of 5-6 mg/kg. Hypotension can be treated with vasopressors, although epinephrine should be avoided as it can lower the pressure further.
If necessary, intubation and assisted breathing may be used. The use of analeptics is not recommended as they could induce seizures.

Biodramina Infantil Leaflet 12.5 Mg 12 Single-dose Envelopes Oral Solution 2.5 Ml