Nasodyne (with Promethazine Carbocisteine)
Nasodyne (with Promethazine Carbocisteine) Uses, Dosage, Side Effects, Food Interaction and all others data.
Carbocisteine reduces goblet cell hyperplasia and therefore plays a role in the management of disorders characterised by abnormal mucous. Carbocisteine loosens thick sputum effectively by reducing its viscosity and thereby helps to expectorate that mucus more easily from the respiratory tract. The mucolytic action happens in several mechanisms. It breaks the disulphide bonds, which cross-link certain glycoprotein molecules in the mucus, the mucus produced under the influence of Carbocisteine has high sialomucin and low fucomucin content. This combined effect ultimately reduces the viscosity of the sputum and increases its volume.
Due to its mucolytic effects, carbocisteine significantly reduces sputum viscosity, cough, dyspnea and fatigue. Additionally, it prevents pulmonary infections by decreasing accumulated mucus in the respiratory tract; this is especially beneficial in preventing exacerbations of COPD caused by bacteria and viruses. It has in-vitro anti-inflammatory activity with some demonstrated action against free radicals.
Promethazine Theoclate works by stopping histamine from binding to its receptors in an area in the brain known as the vomiting centre. The vomiting centre is responsible for causing feelings of sickness and for the vomiting reflex. It is activated when it receives nerve messages from the vestibular apparatus in the middle ear.
The vestibular apparatus provides constant feedback to the brain about the position of our body. When something disturbs the vestibular apparatus, such as movements of the head when travelling by boat or car, nerve signals are sent from the vestibular apparatus to the vomiting centre. This can cause the symptoms of motion sickness, such as nausea, dizziness or spinning sensations (vertigo) and vomiting.
By blocking the histamine receptors in the vomiting centre, Promethazine Theoclate prevents disturbances in the middle ear from activating the vomiting centre.
Promethazine is is a histamine H1 antagonist that can be used for it's ability to induce sedation, reduce pain, and treat allergic reactions. Promethazine's effects generally last 4-6h but can last up to 12h. Patients should be counselled regarding CNS and respiratory depression, reduce seizure threshold, and bone marrow depression.
| Trade Name | Nasodyne (with Promethazine Carbocisteine) |
| Generic | Promethazine + Carbocisteine |
| Weight | 0mg |
| Type | Syrup |
| Therapeutic Class | |
| Manufacturer | May & Baker Nig Plc |
| Available Country | Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Carbocisteine is used for- Acute bronchitis, Chronic bronchitis, Bronchial asthma, Upper respiratory tract inflammation (pharyngitis, laryngitis), Cystic fibrosis Bronchiectasis, Pulmonary tuberculosis, Drainage in chronic sinusitis and pneumonia, Drainage in otitis media in children.
Promethazine Theoclate Tablets are an anti-emetic (anti-sickness drug) which helps to prevent, and treat nausea and vomiting, including travel sickness, and vertigo. Promethazine Theoclate contains promethazine which belongs to a group of medicines called phenothiazines. Your doctor may prescribe this medicine for giddiness or light-headedness (vertigo), or for sickness after an operation, and in such cases the tablets should be taken as instructed by your doctor.
Nasodyne (with Promethazine Carbocisteine) is also used to associated treatment for these conditions: Cough, Respiratory Illness, Excess mucus or phlegm, Airway secretion clearance therapyAllergic urticaria, Anaphylaxis, Cough, Dermographism, Motion Sickness, Nasal Congestion, Postoperative pain, Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Vasomotor Rhinitis, Acute Allergic Reactions, Dry cough, Perioperative nausea and vomiting, Upper respiratory symptoms, Sedative therapy, Adjunct to anesthesia and analgesia
How Nasodyne (with Promethazine Carbocisteine) works
The hypersecretion of mucus characterizes serious respiratory conditions including asthma, cystic fibrosis (CF), and chronic obstructive pulmonary disease (COPD). It blocks bacterial adherence to cells, preventing pulmonary infections. Glycoproteins (fucomucins, sialomucins and sulfomucins) regulate the viscoelastic properties of bronchial mucus. Increased fucomucins can be found in the mucus of patients with COPD. Carbocisteine serves to restore equilibrium between sialomucins and fucomucins, likely by intracellular stimulation of sialyl transferase enzyme, thus reducing mucus viscosity.
A study found that L-carbocisteine can inhibit damage to cells by hydrogen peroxide (H2O2) by activating protein kinase B (Akt) phosphorylation, suggesting that carbocisteine may have antioxidant effects and prevent apoptosis of lung cells. There is some evidence that carbocisteine suppresses NF-κB and ERK1/2 MAPK signalling pathways, reducing TNF-alpha induced inflammation in the lungs, as well as other inflammatory pathways. An in-vitro study found that L-carbocisteine reduces intracellular adhesion molecule 1 (ICAM-1), inhibiting rhinovirus 14 infection, thereby reducing airway inflammation.
Promethazine is a an antagonist of histamine H1, post-synaptic mesolimbic dopamine, alpha adrenergic, muscarinic, and NMDA receptors. The antihistamine action is used to treat allergic reactions. Antagonism of muscarinic and NMDA receptors contribute to its use as a sleep aid, as well as for anxiety and tension. Antagonism of histamine H1, muscarinic, and dopamine receptors in the medullary vomiting center make promethazine useful in the treatment of nausea and vomiting.
Dosage
Nasodyne (with Promethazine Carbocisteine) dosage
Adult: Initially, 2.25 g daily in divided doses, then 1.5 g daily in divided doses as condition improves.
Child: 2-5 year: 62.5-125 mg 4 times daily; 6-12 year 250 mg tid.
Should be taken with food.
To prevent travel sickness on short journeys: Promethazine Theoclate should be taken at least one or two hours before travelling. Adults and children aged over 10 yearsshould take one tablet. Children aged 5 to 10 years should be given half a tablet.
To prevent travel sickness onlong journeys: Promethazine Theoclate should be taken at bedtime each night during the journey, startingthe night before you travel.Adults and childrenaged over 10 yearsshould take one tablet.Children aged 5 to 10 years should be given half a tablet.
To treat travel sickness:Adults and children over 10 years should take one tablet as soon as you feel sick, followed by a second tablet the same evening. Take a third tablet the following evening if necessary. Children aged 5 to 10 years should treated in the same way, but with half a tablet each time.
For sickness and vomiting due to other causes, and for treating vertigo: Adults and children aged over 10 years should take one tablet up to three times aday. Children aged 5 to 10 years should be given half a tablet up to three times a day.Alternativelyyou should follow the instructions given by your doctor.
Side Effects
Gastrointestinal discomfort, nausea, diarrhoea, gastrointestinal bleeding, palpitation, dizziness, headache, heartburn and skin rash may occur.
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with promethazine. Just because a side effect is stated here does not mean that all people using Promethazine Theoclate will experience that or any side effect.
- Drowsiness or feeling tired.
- Dizziness.
- Restlessness.
- Headache.
- Nightmares.
- Blurred vision.
- Difficulty passing urine.
- Dry mouth.
- Confusion.
- Feeling disorientated.
- Unexpected increase in excitability in children.
- Increased sensitivity of the skin to sunlight (photosensitivity). If affected you should avoid sun lamps and direct sunlight while you are taking this medicine.
- Loss of appetite.
- Awareness of your heartbeat (palpitations).
- Abnormal heartbeats (arrhythmias).
- Low blood pressure (hypotension).
- Abnormal movements of the hands, legs, face, neck and tongue, eg tremor, twitching, rigidity (extrapyramidal effects).
- Blood disorders.
Toxicity
The oral LD50 of carbocisteine in rats is >15000 mg/kg. An overdose with carbocisteine is likely to result in gastrointestinal discomfort with nausea and vomiting.
The intraperitoneal LD50 in rats is 170mg/kg and in mice is 160mg/kg. The subcutaneous LD50 in rats is 400mg/kg and in mice is 240mg/kg. The oral LD50 in mice is 255mg/kg.
Patients experiencing an overdose of promethazine may present with mild central nervous system and cardiovascular depression, hypotension, respiratory depression, unconciousness, hyperreflexia, hypertonia, ataxia, athetosis, extensor-plantar reflexes, convulsions, dry mouth, flushing, gastrointestinal symptoms, and fixed, dilated pupils. Treat overdoses with symptomatic and supportive treatment, which may include activated charcoal, sodium sulfate, magnesium sulfate, controlled ventilation, diazepam, intravenous fluids, vasopressors, norepinephrine, phenylephrine, anticholinergic antiparkinsonian agents, diphenhydramine, barbiturates, or oxygen.
Precaution
No specific precaution is recommended but Carbocisteine should be used with caution in patients with a recent history of peptic ulcer and recurrent gastrointestinal bleeding.
Promethazine Theoclate tablets can make some people feel drowsy, dizzy, confused or disorientated and this may reduce your ability to drive or operate machinery safely. Do not drive or operate machinery until you know how this medicine affects you and you are sure it won't affect your performance. If your child is affected in this way they should avoid potentially hazardous activities such as riding bikes. You should not leave your child unattended after giving them this medicine.
Avoid drinking alcohol while taking Promethazine Theoclate because this is likely to make the above effects more likely or worse.
Promethazine Theoclate tablets may make your skin more sensitive to sunlight than usual, so you should avoid exposing your skin to direct sunlight or sunlamps until you know how your skin reacts. If you can't avoid strong sunlight you should use a sunscreen lotion or make sure your skin is protected with clothing.
This medicine may interfere with some pregnancy tests, causing false negative or false positive results.
If you are due to have any skin prick tests to diagnose allergies you should stop taking Promethazine Theoclate at least 72 hours before the tests. This is because antihistamines can prevent or lessen the skin reactions that indicate an allergy, and so can make the test results unreliable.
Interaction
Neither hazardous nor therapeutically useful interactions have been reported.
It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start taking Promethazine Theoclate. Similarly, check with your doctor or pharmacist before taking any new medicines while taking Promethazine Theoclate, to make sure that the combination is safe.
Promethazine Theoclate should not be taken by anyone who has taken a type of antidepressant called a monoamine oxidase inhibitor (MAOI), eg phenelzine, tranylcypromine, isocarboxazid, in the previous 14 days.
You are more likely to feel drowsy if you take Promethazine Theoclate with any of the following (which can also cause drowsiness):
- alcohol
- antipsychotic medicines, eg chlorpromazine
- barbiturates, eg phenobarbital
- benzodiazepines, eg diazepam, temazepam
- sedating antihistamines, eg chlorphenamine, brompheniramine, hydroxyzine
- sleeping tablets, eg zopiclone
- strong opioid painkillers, eg morphine, codeine, dihydrocodeine, tramadol
- tricyclic antidepressants, eg amitriptyline.
Volume of Distribution
Carbocisteine penetrates well into the lung and bronchial secretions.
The volume of distribution of promethazine is approximately 970L or 30L/kg.
Elimination Route
Carbocisteine is rapidly absorbed in the gastrointestinal tract when taken orally with peak serum concentrations achieved within 1 to 1.7 hours.
A 25mg dose of intramuscular promethazine reaches a Cmax of 22ng/mL. Intravenous promethazine reaches a Cmax of 10.0ng/mL, with a Tmax of 4-10h, and an AUC of 14,466ng*h/mL. Oral promethazine is only 25% bioavailable due to first pass metabolism. Oral promethazine reaches a Cmax of 2.4-18.0ng/mL, with a Tmax of 1.5-3h, and an AUC of 11,511ng*h/mL.
Half Life
The plasma half-life of carbicostine is 1.33 hours.
The elimination half life of promethazine is approximately 12-15h.
Clearance
Clearance information for carbocisteine is not readily available in the literature.
The intravenous clearance of promethazine is approximately 1.14L/min. The renal clearance of promethazine is 5.9mL/min and the renal clearance of promethazine sulfoxide is 90.4mL/min.
Elimination Route
About 30% to 60% of an orally administered dose is detected unchanged in the urine.
An intravenous dose of promethazine is 0.64% eliminated in the urine as the unchanged parent drug, 0.02-2.02% in the urine as desmethylpromethazine, 10% in the urine as promethazine sulfoxide.
Pregnancy & Breastfeeding use
There is no information on the use of Carbocisteine during lactation. While there are no reports of teratogenic effects, the manufacturers do not recommend the use of Carbocisteine in the first trimester.
If you are pregnant you should not take Promethazine Theoclate without consulting your doctor first. Promethazine Theoclate should only be used during pregnancy if essential, and only if the expected benefit to the mother outweighs any potential risks to the developing baby. It should not be used during the last two weeks of pregnancy, because if taken during this time it may cause irritability or excitement in the baby after birth. Seek further medical advice from your doctor.
Small amounts of Promethazine Theoclate may pass into breast milk. This is not expected to be harmful to a nursing infant with occasional short-term use of Promethazine Theoclate, but there is a risk that it may cause drowsiness, irritability or excitement in a newborn baby. If you are breastfeeding you should not take Promethazine Theoclate without getting medical advice from your doctor first.
Contraindication
Contraindicated in active peptic ulceration and in patients with hypersensitivity to the drug.
- Children under five years of age.
- People with reduced awareness, slow reactions or extreme drowsiness caused by medicines or illnesses that reduce activity in the central nervous system.
- People who have taken a type of medicine called a monoamine-oxidase inhibitor antidepressant (MAOI) in the past 14 days.
- Children and adolescents who have signs and symptoms suggestive of Reye's syndrome.
- People who are allergic to any ingredients of the tablets.
- Promethazine Theoclate tablets contain lactose and should not be taken by people with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.
Acute Overdose
Symptoms: GI disturbance.
Management: May perform gastric lavage, followed by observation.
Storage Condition
Store in a cool and dry place protected from light.
Store between 15-30° C. Protect from light.
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