Doxylamine Pharmacology

In the podcast this week, I talk about doxylamine pharmacology. Doxylamine is a first-generation antihistamine; it is commonly an active ingredient in night-time medications like Unisom, Nyquil, and Mucinex. The pharmacology of doxylamine is similar to other first-generation antihistamines, it competitively inhibits the binding of histamine at H1 receptors. Its main uses are as sleep aides, in cough-and-cold medications, but doxylamine has also been given with pyridoxine to treat nausea and vomiting during pregnancy.

Doxylamine’s adverse reactions are related to its anticholinergic properties, they include dry eyes, dry mouth, increased fall risk, sedation, urinary retention, constipation, and confusion. Contraindications include concurrent use with a monoamine oxidase inhibitor, known hypersensitivities, concomitant alcohol use, and if the patient has the following conditions: elevated intraocular pressure, narrow-angle glaucoma, asthma, peptic ulcer disease, urinary bladder neck obstruction, or gastric outlet obstruction. It is also a Beer’s list drug due to its anticholinergic effects. The normal dose in adults is 25 mg. In cases of overdosage, the most common manifestation is exacerbations of its anticholinergic effects. The major complications of an overdose include arrhythmia, respiratory failure, seizures, hyperthermia, rhabdomyolysis, and coma. 

When you know a patient is taking doxylamine, it’s important to be cognizant of their occupation, as well as what other conditions they may have. For example, doxylamine should be used with caution in patients that drive heavy machinery due to its sedating properties. You might be able to tell if a patient’s experiencing an adverse reaction exacerbation if they begin having worsening dementia symptoms or increased urinary retention. Other indications include the use of artificial tears, or saliva, or increased complaints of constipation. To monitor for doxylamine, it’s important to monitor the patient’s tolerability. The onset of doxylamine is relatively quick as well, with a peak concentration within 2-4 hours.

For drug-drug interactions, CYP interactions aren’t as concerning as usual. The main interaction to consider when a patient is taking doxylamine is additive anticholinergic effects. Sedative effects can increase when benzodiazepines, skeletal muscle relaxants, opioids, or antihistamines are concurrently taken. Doxylamine can also counteract the usefulness of dementia or BPH medications due to its anticholinergic properties. There is also a risk of increased anticholinergic burden when taken with skeletal muscle relaxants or tricyclic antidepressants. 

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Show notes provided by Chong Yol G Kim, PharmD Student.

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Cetirizine Pharmacology

On this episode of the Real Life Pharmacology Podcast, I discuss cetirizine pharmacology.

Cetirizine, commonly known as Zyrtec, is a 2nd generation antihistamine. Compared to 1st generation antihistamines, like diphenhydramine and chlorpheniramine, 2nd generation antihistamines have fewer anticholinergic effects. Pharmacologically, cetirizine works by selectively blocking histamine from binding to the H1 receptor. The uses for cetirizine are allergic rhinitis, itching, and sometimes acute allergic reactions. Commonly, cetirizine is dosed at 10 mg daily, and can even be escalated to 10 mg twice daily in rare situations. In adults 77 years old and older, the manufacturer recommended dose tops out at 5 mg daily. There are also liquid and chewable formulations for children. 

The adverse drug reactions cetirizine are mostly dose-dependent and related to its pharmacology. Out of all of the 2nd generation antihistamines, like fexofenadine and loratadine, cetirizine is the most sedating. Other adverse drug reactions related to its anticholinergic effects are urinary retention, constipation, confusion, fatigue, and dizziness. Lab monitoring is not necessary when taking cetirizine. It is important to monitor the adverse drug reactions when taking cetirizine, as well as improvement in the signs and symptoms of what it’s used for. 

Cetirizine does not undergo metabolism through liver CYP enzymes, so drug-drug interactions involving those enzymes are uncommon. The interactions that are concerning are additive effects of cetirizine’s adverse drug reactions. Drowsiness can be compounded when cetirizine is taken with opioids, sleep medications, alcohol, or other older anticholinergics with sedative effects. There is also a risk of an increased anticholinergic burden when taking medications like Cogentin, oxybutynin, TCAs, and inhaled anticholinergics. 

The manifestation of overdoses will vary depending on age. In adults, the most common observation made was sedation and somnolence. In children, restlessness and irritability were observed initially, then drowsiness. Cetirizine is not removed by dialysis. When treating overdoses, the symptoms that manifest should be treated.  

Show notes provided by Chong Yol G Kim, PharmD Student.

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Doxepin Pharmacology

Doxepin is under the class of tricyclic antidepressants. It can inhibit the reuptake of serotonin and norepinephrine.

In addition to the serotonin and norepinephrine reuptake inhibition mechanism, doxepin also has antihistamine type effects.

Because of the anticholinergic activity of doxepin, it is recommended to avoid this medication in the elderly, particularly at high doses.

Be aware that anticholinergics like doxepin can reduce the benefit of dementia medications.

CYP2D6 is an important enzyme in the metabolism of doxepin and drugs like bupropion that inhibit CYP2D6 can increase the concentrations of doxepin.

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