Homatropine And Hydrocodone

Homatropine And Hydrocodone Uses, Dosage, Side Effects, Food Interaction and all others data.

Homatropine, a tertiary amine antimuscarinic, produces dilation and loss of accommodation by blocking the response of iris sphincter muscle and the accommodative ciliary muscle to cholinergic stimulation.

Homatropine is an anticholinergic drug that produces typical anticholinergic effects inducing mydriasis and cycloplegia. Other effects of structurally-related atropine that could also apply to homatropine include inhibition of secretions, tachycardia, relaxation of smooth muscle and central nervous effects including excitation .

Hydrocodone is a synthetic opioid derivative of codeine. It is commonly used in combination with acetaminophen to control moderate to severe pain. Historically, hydrocodone has been used as a cough suppressant although this has largely been replaced by dextromethorphan in current cough and cold formulations. Hydrocodone's more potent metabolite, hydromorphone has also found wide use as an analgesic and is frequently used in cases of severe pain. The FDA first approved Hydrocodone for use as part of the cough suppressant syrup Hycodan in March of 1943.

Hydrocodone inhibits pain signaling in both the spinal cord and brain . Its actions in the brain also produce euphoria, respiratory depression, and sedation.

Trade Name Homatropine And Hydrocodone
Generic Homatropine + hydrocodone
Weight 1.5mg + 5mg/5ml, 1.5mg + 5mg
Type Oral syrup, oral tablet
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Homatropine And Hydrocodone
Homatropine And Hydrocodone

Uses

Homatropine Hydrobromide sterile Eye Drops is used for use as a mydriatic and cycloplegic agent.

Hydrocodone is an opioid agonist used as an analgesic and antitussive agent.

Hydrocodone is indicated for the management of acute pain, sometimes in combination with acetaminophen or ibuprofen, as well as the symptomatic treatment of the common cold and allergic rhinitis in combination with decongestants, antihistamines, and expectorants.

Homatropine And Hydrocodone is also used to associated treatment for these conditions: StrabismusCough, Cough caused by Allergic Rhinitis, Cough caused by Common Cold, Nasal Congestion caused by Allergic Rhinitis, Nasal Congestion caused by Common Cold, Pain, Acute, Pain, Chronic, Rhinitis caused by Common Cold, Severe Pain, Moderate Pain, Upper respiratory symptoms caused by Allergic Rhinitis, Upper respiratory symptoms caused by Common Cold

How Homatropine And Hydrocodone works

Homatropine is a competitive muscarinic receptor antagonist with a bulky aromatic group in place of the acetyl group of acetylcholine. It is expected to act in similar manner as atropine, producing similar parasympatholytic effects. By blocking muscarinic receptors and cholinergic signalling pathways, homatropine blocks the response of the iris sphincter muscle and cause the pupil to become unresponsive to light upon dilation or mydriasis. It also blocks the accommodative muscle of the ciliary body to cholinergic stimulation .

Hydrocodone binds to the mu opioid receptor (MOR) with the highest affinity followed by the delta opioid receptors (DOR). Hydrocodone's agonist effect at the MOR is considered to contribute the most to its analgesic effects. Both MOR and DOR are Gi/o coupled and and produces its signal through activation of inward rectifier potassium (GIRK) channels, inhibition of voltage gated calcium channel opening, and decreased adenylyl cyclase activity. In the dorsal horn of the spinal cord, activation of pre-synaptic MOR on primary afferents the inhibition of calcium channel opening and increased activity of GIRK channels hyperpolarizes the neuron and prevents release of neurotransmitters. Post-synaptic MOR can also prevent activation of neurons by glutamate through the aforementioned mechanisms.

Hydrocodone can also produce several actions in the brain similarly to other opioids. Activation of MOR in the periaquaductal gray (PAG) inhibits the GABAergic tone on medulo-spinal neurons. This allows these neurons, which project to the dorsal horn of the spinal cord, to suppress pain signalling in secondary afferents by activating inhibitory interneurons. MOR can also inhibit GABAergic neurons in the ventral tegmental area, removing the inhibitory tone on dopaminergic neurons in the nucleus accumbens and contributing to the activation of the brain's reward and addiction pathway. The inhibitory action or MOR likely contributes to respiratory depression, sedation, and suppression of the cough reflex.

Activation of DOR may contribute to analgesia through the above mechanisms but has not been well studied.

Dosage

Homatropine And Hydrocodone dosage

Mydriasis and cycloplegia for refraction:

  • Adult: Instill 1 or 2 drops of 2% solution, or 1 drop of 5% solution immediately before the procedure, repeat at 5-10 minute intervals if necessary.
  • Child: Instill 1 drop of 2% soln immediately before the procedure, repeat at 10-min intervals if necessary.

Uveitis:

  • Adult: Instill 1-2 drops of 2% or 5% solution bid-tid up to every 3-4 hr as needed.
  • Child: 3 mth- 2 yr: instill 1 drop of 0.5% soln once daily or on alternate days. >2 yr: instill 1 drop of 1% or 2% soln bid.

Side Effects

Hypersensitivity may occur as conjunctivitis.

Toxicity

Acute oral LD50 is 1200 mg/kg in rat, 1400 mg/kg in mouse, and 1000 mg/kg in guinea pig . Systemic toxicity may occur following topical overdose of structurally-related ophthalmic atropine, particularly in children. It is characterized by flushing and dryness of the skin, blurred vision, a rapid and irregular pulse, fever, convulsions and hallucinations, and the loss of neuromuscular coordination. Abdominal distension may be observed with infants. Severe intoxication is manifested by central nervous system depression, coma, circulatory and respiratory failure, and death . Symptomatic and supportive treatment should be initiated. In case of accidental use or overdose in infants and small children, the body surface should be kept moist .

Overdosage with hydrocodone presents as opioid intoxication including respiratory depression, somnolence, coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death.

In case of oversdosage the foremost priority is the maintenance of a patent and protected airway with the provision of assisted ventilation if necessary. Supportive measures such as IV fluids, supplemental oxygen, and vasopressors may be used to manage circulatory shock. Advanced life support may be necessary in the case of cardiac arrest or arrhythmias. Opioid antagonists such as naloxone may be used to reverse the respiratory and circulatory effects of hydrocodone. Emergency monitoring is still required after naloxone administration as the opioid effects may reappear. Additionally, if used in an opioid tolerant patient, naloxone may produce opioid withdrawal symptoms.

Precaution

Should be used with caution in patients with prostatic enlargement and in patients suffering from paralytic ileus or pyloric stenosis.

Interaction

Effects may be increased by drugs with antimuscarinic effect such as; some antihistamines; phenothiazines; antipsychotics; TCAs; MAOIs or parasympathomimetics.

Volume of Distribution

No pharmacokinetic data available.

The apparent volume of distribution ranges widely in published literature. The official FDA labeling reports a value of 402 L. Pharmacokinetic studies report values from 210-714 L with higher values associated with higher doses or single dose studies and lower values associated with lower doses and multiple dose studies. Hydrocodone has been observed in human breast milk at levels equivalent to 1.6% of the maternal dosage. Only 12 of the 30 women studied had detectable concentrations of hydromorphone at mean levels of 0.3 mcg/kg/day.

Elimination Route

No pharmacokinetic data available.

The absolute bioavailability of hydrocodone has not been characterized due to lack of an IV formulation. The liquid formulations of hydrocodone have a Tmax of 0.83-1.33 h. The extended release tablet formulations have a Tmax of 14-16 h. The Cmax remains dose proportional over the range of 2.5-10 mg in liquid formulations and 20-120 mg in extended release formulations. Administration with food increases Cmax by about 27% while Tmax and AUC remain the same. Administration with 40% ethanol has been observed to increase Cmax 2-fold with an approximate 20% increase in AUC with no change in Tmax. 20% alcohol produces no significant effect.

Half Life

No pharmacokinetic data available.

The half-life of elimination reported for hydrocodone is 7-9 h.

Clearance

No pharmacokinetic data available.

Official FDA labeling reports an apparent clearance of 83 L/h. Pharmacokinetic studies report values ranging from 24.5-58.8 L/h largely dependent on CYP2D6 metabolizer status.

Elimination Route

No pharmacokinetic data available.

Most hydrocodone appears to be eliminated via a non-renal route as renal clearance is substantially lower than total apparent clearance. Hepatic metabolism may account for a portion of this, however the slight increase in serum concentration and AUC seen in hepatic impairment indicates a different primary route of elimination.

Pregnancy & Breastfeeding use

Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Matropin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Use in lactation: It is not known whether Homatropine is excreted in human milk. Caution should be exercised when Matropin is administered to a nursing mother.

Contraindication

Contraindicated in patients with closed-angle glaucoma or with a narrow angle between the iris and the cornea.

Special Warning

Use in children: Should not be used in children below the age of 3 months

Acute Overdose

Ataxia, incoherent speech, restlessness, hallucinations, disorientation, failure to recognize people and tachycardia. Psychotic reactions and behavioural disturbances (in children). SC/IM/IV Physostigmine salicylate 1-2 mg to control central and peripheral effects. Small doses of short-acting barbiturate eg. thiopentone sodium 100 mg to control excitement.

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