Oxynil

Uses

Copper is a transition metal found in a variety of supplements and vitamins, including intravenous solutions for total parenteral nutrition (TPN).

For use in the supplementation of total parenteral nutrition and in contraception with intrauterine devices .

• Perenial and seasonal allergic rhinitis
• Vasomotor rhinitis
• Allergic conjunctivitis due to inhalant allergens and foods
• Mild, uncomplicated allergic skin manifestations of urticaria and angioedema
• Amelioration of allergic reactions to blood or plasma
• Cold urticaria
• Dermatographism

As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled.

Oxynil is also used to associated treatment for these conditions: Emergency Contraception, IUD, Trace Element Deficiency, Dietary supplementationAllergic Reactions caused by Transfusions, Anaphylaxis, Angioedema and urticaria, Cold urticaria, Conjunctivitis allergic caused by Food Allergy, Conjunctivitis allergic caused by inhalant allergens, Perennial Allergic Rhinitis (PAR), Pruritus, Seasonal Allergic Rhinitis, Serotonin Syndrome, Vasomotor Rhinitis, Dermatographism, Appetite stimulation

How Oxynil works

Copper is absorbed from the gut via high affinity copper uptake protein and likely through low affinity copper uptake protein and natural resistance-associated macrophage protein-2 . It is believed that copper is reduced to the Cu1+ form prior to transport. Once inside the enterocyte, it is bound to copper transport protein ATOX1 which shuttles the ion to copper transporting ATPase-1 on the golgi membrane which take up copper into the golgi apparatus. Once copper has been secreted by enterocytes into the systemic circulation it remain largely bound by ceruloplasmin (65-90%), albumin (18%), and alpha 2-macroglobulin (12%).

Copper is an essential element in the body and is incorporated into many oxidase enzymes as a cofactor . It is also a component of zinc/copper super oxide dismutase, giving it an anti-oxidant role. Copper defiency occurs in Occipital Horn Syndrome and Menke's disease both of which are associated with impaired development of connective tissue due to the lack of copper to act as a cofactor in protein-lysine-6-oxidase. Menke's disease is also associated with progressive neurological impairment leading to death in infancy. The precise mechanisms of the effects of copper deficiency are vague due to the wide range of enzymes which use the ion as a cofactor.

Copper appears to reduce the viabilty and motility of spermatozoa . This reduces the likelihood of fertilization with a copper IUD, producing copper's contraceptive effect . The exact mechanism of copper's effect on sperm are unknown.

Cyproheptadine appears to exert its antihistamine and antiserotonin effects by competing with free histamine and serotonin for binding at their respective receptors. Antagonism of serotonin on the appetite center of the hypothalamus may account for cyproheptadine's ability to stimulate the appetite.

Dosage

Oxynil dosage

Pediatric Patients:Age 2 To 6 Years:

• The total daily dosage for pediatric patients may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day or 8 mg per square meter of body surface (8 mg/m2).
• The usual dose is 2 mg two or three times a day, adjusted as necessary to the size and response of the patient. The doe is not to exceed 12 mg a day.

Age 7 To 14 Years:

• The usual dose is 4 mg two or three times a day adjusted as necessary to the size and response of the patient. The dose is not to exceed 16 mg a day.

Adults: The total daily dose for adults should bot exceed 0.5 mg/kg/day. The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 to 16 mg a day. An occasional patient may require as much as 32 mg a day for adequate relief. It is suggested that dosage be initiated with 4 mg three times a day and adjusted according to the size and response of the patient.

Side Effects

Confusion, disturbed coordination, dizziness, excitation, euphoria, hallucinations, headache, hysteria, insomnia, irritability, nervousness, restlessness, sedation, seizure, sleepiness, tremor, vertigo, hypotension, palpitation, tachycardia, abdominal pain, anorexia, increased appetite, constipation, diarrhoea, nausea, vomiting, xerostomia, difficult urination, urinary retention, urinary frequency, blurred vision, diplopia, tinnitus, acute labyrinthitis, nasal congestion, pharyngitis, thickening bronchial secretion, paraesthesia, hepatitis, cholestasis, hepatic failure, jaundice, angioedema, photosensitivity, rash, urticaria, fatigue, chills, diaphoresis.

Toxicity

Copper toxicity is belevied to be due to fenton-type redox reactions occuring with high copper concentrations which produce damaging reactive oxygen species .

Overdosage with cyproheptadine is likely to result in significant sedation - although paradoxical stimulation has been noted in pediatric patients - and anticholinergic adverse effects such as dry mouth and flushing. Most patients appear to recover without incident, as a review of cyproheptadine overdose cases in Hong Kong found the majority of patients had no or mild symptoms following intentional overdose.

In the event of overdosage with cyproheptadine, prescribing information recommends the induction of vomiting (if it has not occurred spontaneously) using syrup of ipecac. Gastric lavage and activated charcoal may also be considered. Vasopressors may be used to treat hypotension and intravenous physostigmine salicylate may be considered for the treatment of significant CNS symptoms depending on the clinical picture.

Precaution

Patient with CV disease including HTN and ischaemic heart disease, increased intraocular pressure, asthma or other chronic breathing disorders, thyroid dysfunction. Pregnancy.

Interaction

May have additive effects with CNS depressants e.g. hypnotics, sedatives, tranquilizers, antianxiety agents. MAOIs prolong and intensify the anticholinergic effects of antihistamines.

Elimination Route

Copper absorption varies inversely with intake. Absorption range is 12-65%.

A single study examining the difference in absorption of orally administered versus sublingually administered cyproheptadine in five healthy males demonstrated a mean C_max of 30.0 mcg/L and 4.0 mcg/L, respectively, and a mean AUC of 209 mcg.h/L and 25 mcg.h/L, respectively. The T_max of orally and sublingually administered cyproheptadine was 4 hours and 9.6 hours, respectively.

Elimination Route

Copper appears to be eliminated primarily through bile .

Approximately 2-20% of the radioactivity from an orally administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose). At least 40% of radioactivity is recovered in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Narrow-angle glaucoma, bladder neck obstruction, pyloroduodenal obstruction, symptomatic prostatic hyperplasia, stenosing peptic ulcer. Concurrent use with MAOIs. Debilitated elderly, newborn or premature infants. Lactation.

Acute Overdose

Symptoms: CNS depression to stimulation, atropine-like (e.g. dry mouth, fixed, dilated pupils, flushing) and GI symptoms.

Management: Induce vomiting with syrup of ipecac. If unable to vomit, perform gastric lavage followed by activated charcoal. Saline cathartics may be useful for quick dilution of bowel content by osmosis. Vasopressors may be used for hypotension.

Storage Condition

Store between 15-30°C.

Innovators Monograph

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