Navigation

Optimin

Optimin - General Information

A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (histamine H1 antagonists) it lacks central nervous system depressing effects such as drowsiness. [PubChem]

 

Pharmacology of Optimin

Optimin, a non-sedating H1-blocker similar in structure to cyproheptadine and azatadine, is used to treat seasonal allergic rhinitis. Unlike other H1-blockers, loratidine does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.

 

Optimin for patients

Description
--------------------------------------------------------------------------------

This medicine is used to treat symptoms of hay fever such as runny nose,
watery eyes and sneezing. Your doctor may use antihistimines for other
conditions as well.

General Information
--------------------------------------------------------------------------------

This information is for educational purposes only. Not every known side
effect, adverse effect, or drug interaction is in this database. If you
have questions about your medicines, talk to your healthcare provider.

Proper use of this medicine
--------------------------------------------------------------------------------

For proper use of this medicine, follow the directions on the package,
unless otherwise instructed by your doctor.

Missed Dose
--------------------------------------------------------------------------------

If your doctor has instructed you to take this medicine regularly and you
miss a dose, take your next dose, as soon as you remember. If you are close
to your next dose, do not double up. Skip the missed dose and go back to
your regular schedule.

Storage
--------------------------------------------------------------------------------

Keep this medication in the container it came in, tightly closed, and out
of reach of children. Store it at room temperature and away from excess
heat and moisture (not in the bathroom). Throw away any medication that
is outdated or no longer needed.

Possible Side Effects
--------------------------------------------------------------------------------

Common side effects include:
dizzines
drowsiness
dry mouth
This medicine can cause excitement especially in children.
See a doctor immediately if you experience:
fast or irregular heartbeat
mental or mood changes
tightness in the chest
unusual tiredness or weakness.
While taking this medicine, if you experience, chest tightness, difficulty
in breathing or swallowing, swelling in the face or lips, go to the doctor
immediately and stop taking the medication until you have talked to your
doctor.

Warnings/Precautions
--------------------------------------------------------------------------------

Do NOT take this medicine with orange, apple or grapefruit juice. The levels
of this medicine in your blood may be decreased by 70%.

Overdose
--------------------------------------------------------------------------------

Seek medical attention immediately. For non emergencies, contact your local
or regional poison control center

Drug Interactions
--------------------------------------------------------------------------------

Before taking any other medications, by prescription or over-the-counter
(OTC) talk to your health care provider. Some medicines may change the way
this medicine affects your body. Also the effects of other medicines may
be increased or decreased by this medicine.

Pregnancy/Nursing
--------------------------------------------------------------------------------

Talk to your doctor about using this medicine during pregnancy or nursing
to discuss any possible risks to you or your baby.

More Information
--------------------------------------------------------------------------------

For more information about this medicine, talk to your healthcare provider

 

Optimin Interactions

Loratadine (10 mg once daily) has been coadministered with therapeutic doses of erythromycin, cimetidine, and ketoconazole in controlled clinical pharmacology studies in adult volunteers. Although increased plasma concentrations (AUC 0-24 hrs) of loratadine and/or descarboethoxyloratadine were observed following coadministration of loratadine with each of these drugs in normal volunteers (n = 24 in each study), there were no clinically relevant changes in the safety profile of loratadine, as assessed by electrocardiographic parameters, clinical laboratory tests, vital signs, and adverse events. There were no significant effects on QTc intervals, and no reports of sedation or syncope. No effects on plasma concentrations of cimetidine or ketoconazole were observed. Plasma concentrations (AUC 0-24 hrs) of erythromycin decreased 15% with coadministration of loratadine relative to that observed with erythromycin alone. The clinical relevance of this difference is unknown. These above findings are summarized in TABLE 1.

TABLE 1 Effects on Plasma Concentrations (AUC 0-24 hrs) of Loratadine and Descarboethoxyloratadine After 10 Days of Coadministration (Loratadine 10 mg) in Normal Volunteers
  Loratadine Descarboethoxyloratadine
 Erythromycin (500 mg q8h) + 40% +46%
 Cimetidine (300 mg qid) +103% + 6%
 Ketoconazole (200 mg q12h) +307% +73%


There does not appear to be an increase in adverse events in subjects who received oral contraceptives and loratadine.

 

Optimin Contraindications

Loratadine is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.

 

Additional information about Optimin

Optimin Indication: For the relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and for the treatment of chronic idiopathic urticaria in patients 2 years of age or older
Mechanism Of Action: Like other H1-blockers, loratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Optimin also has a weak affinity for acetylcholine and alpha-adrenergic receptors.
Drug Interactions: Nefazodone Increased risk of cardiotoxicity
Food Interactions: Take on empty stomach: 1 hour before or 2 hours after meals.
Generic Name: Loratadine
Synonyms: Loratadina [Spanish]; Loratadinum [Latin]
Drug Category: Anti-Allergic Agents; Antipruritics; Antihistamines; Histamine H1 Antagonists, Non-Sedating
Drug Type: Small Molecule; Approved

Other Brand Names containing Loratadine: Aerotina; Alarin; Alavert; Alerpriv; Allertidin; Bedix Loratadina; Biloina; Bonalerg; Civeran; Claratyne; Clarinase; Clarinase Reperabs; Claritin; Claritin Reditabs; Claritin-D; Claritine; Clarityn; Clarityne; Fristamin; Histaloran; Lergy; Lertamine; Lesidas; Lisino; Loracert; Loradex; Loradif; Loranox; Lorantis; Lorastine; Loratyne; Loraver; Lorfast; Loritine; Lowadina; Nularef; Optimin; Polaratyne; Pylor; Restamine; Rhinase; Rinomex; Sanelor; Sensibit; Sinhistan Dy; Sohotin; Tadine; Talorat Dy; Velodan; Versal; Zeos; Lomilan; Roletra;
Absorption: Rapidly absorbed following oral administration (40% bioavailability)
Toxicity (Overdose): somnolence, tachycardia, and headache LD50=mg/kg (orally in rat)
Protein Binding: Not Available
Biotransformation: Hepatic
Half Life: 8.4 hours
Dosage Forms of Optimin: Tablet Oral
Syrup Oral
Chemical IUPAC Name: 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
Chemical Formula: C22H23ClN2O2
Loratadine on Wikipedia: https://en.wikipedia.org/wiki/Loratadine
Organisms Affected: Humans and other mammals