Pseudoephedrine

Pseudoephedrine ( Pseudo ephedrine ) (PSE) is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It may be used as a nasal/sinus decongestant, as a stimulant, or as a wakefulness-promoting agent.

The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations, either as a single ingredient or (more commonly) in combination with antihistamines, guaifenesin, dextromethorphan, and/or paracetamol (acetaminophen) or another NSAID (such as aspirin or ibuprofen).

Pharmacokinetics.
Distribution: Distributes into breast milk.
Metabolism: Partially metabolized in the liver.
Elimination: Renal (55% to 75% as unchanged); acidic urine accelerates rate of excretion.
Onset: 15 to 30 min.
Peak: 30 to 60 min.
Duration: 3 to 4 h; 8 to 12 h (extended-release).

 
Dosage and Administration.

Pseudoephedrine Sulfate
Adults and Children older than 12 yr of age 

PO 120 mg sustained-release every 12 h.

Pseudoephedrine Hydrochloride
Adults 

PO 60 mg every 4 to 6 h or 120 mg sustained-release every 12 h. Not to exceed 240 mg/day.

Children. The BNFC states there is little evidence to support the use of systemic decongestants in children. However, the following oral doses of pseudoephedrine hydrochloride are suggested for children in the management of mucosal congestion of the upper respiratory tract:
• 2 to 6 years: 15 mg 3 or 4 times daily
• 6 to 12 years: 30 mg 3 or 4 times daily, Not to exceed 120 mg/day.
Over-the-counter cough and cold preparations containing sympathomimetic decongestants (including pseudoephedrine) should be used with caution in children and generally avoided in those under 2 years of age

Under 4 years of age.  Not approved by FDA because dosage not studied in this age range 

Avoid multi-ingredient products in children under 6 years of age (AAP recommendations 10/2008)

Indications.

• nasal congestion
• sinus congestion
• Eustachian tube congestion
• vasomotor rhinitis
• as an adjunct to other agents in the optimum treatment of allergic rhinitis, croup, sinusitis, otitis media, and tracheobronchitis.
• also used as a first-line prophylactic for recurrent priapism
• urinary incontinence (off-label use)

Adverse effects.

• Common adverse drug reactions (ADRs) associated with pseudoephedrine therapy include: CNS stimulation, insomnia, nervousness, excitability, dizziness and anxiety.
• Infrequent ADRs: tachycardia or palpitations. 
• Rarely, mydriasis (dilated pupils), hallucinations, arrhythmias, hypertension, seizures and ischemic colitis; as well as severe skin reactions known as recurrent pseudo-scarlatina, systemic contact dermatitis, and nonpigmenting fixed drug eruption. 
• Pseudoephedrine, particularly when combined with other drugs including narcotics, may also play a role in the precipitation of episodes of paranoid psychosis. It has also been reported that pseudoephedrine, amongst other sympathomimetic agents, may be associated with the occurrence of stroke.

  A child who suffered a generalised seizure after ingesting a large quantity of pseudoephedrine hydrochloride tablets was believed to be the first report of convulsions associated with overdose of a preparation containing the drug as a single ingredient.
Clark RF, Curry SC. Pseudoephedrine dangers. Pediatrics 1990; 85: 389–90.

Precautions and contraindications.
Not be used in patients with: 

• diabetes mellitus, 
• cardiovascular disease, 
• severe or uncontrolled hypertension, 
• severe coronary artery disease,  
• prostatic hypertrophy, 
• hyperthyroidism, 
• closed angle glaucoma, 
• pregnant women ( Category C ) .
• Do not give to breast-feeding mothers.
   A small, randomised, crossover study concluded that a single dose of 60 mg pseudoephedrine hydrochloride decreased 24-hour milk production by 24%. The authors of the study suggested that pseudoephedrine might be of benefit for suppressing excess milk production.3
  
  1. American Academy of Pediatrics. The transfer of drugs and other chemicals into human milk. Pediatrics 2001; 108: 776–89. Correction. ibid.; 1029.
  2. Findlay JWA, et al. Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers. Br J Clin Pharmacol 1984; 18: 901–6.
  3. Aljazaf K, et al. Pseudoephedrine: effects on milk production in women and estimation of infant exposure via breastmilk. Br J Clin Pharmacol 2003; 56: 18–24.

Patients who are prone to anxiety or panic attacks should use pseudoephedrine with caution, as anxiety and restlessness are common side effects, mostly due to the drug's stimulant properties.

Since nasal congestion is considered to be a relatively minor illness, alternatives are preferred in patients with these conditions. Appropriate alternatives may include saline sprays/instillations, depending on the patient's condition. Topical decongestants should be used with caution and for no longer than three days to avoid rhinitis medicamentosa.

Under 4 years of age. Not approved by FDA because dosage not studied in this age range
Avoid multi-ingredient products in children under 6 years of age (AAP recommendations 10/2008)

Interactions.

• Concomitant or recent (previous fourteen days) monoamine oxidase inhibitor use can lead to hypertensive reactions, including hypertensive crises.
• The antihypertensive effects of methyldopa, mecamylamine, reserpine and veratrum alkaloids may be reduced by sympathomimetics (pseudoephedrine ). 
• Beta-adrenergic antagonists may also interact with sympathomimetics. 
• Increase of ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis. 
• Antacids increase the rate of pseudoephedrine absorption, while kaolin decreases it.

Abuse. 

Acute psychosis and visual and tactile hallucinations have been reported in an 18-year-old male after intravenous misuse of pseudoephedrine hydrochloride. Pseudoephedrine has also been used for the illicit manufacture of street stimulants such as metamfetamine 

Sullivan G. Acute psychosis following intravenous abuse of pseudoephedrine: a case report. J Psychopharmacol 1996; 10: 324–5.

 

Read More:

Martindale; The complete drug reference, 36th edition
Pseudoephedrine | MedlinePlus Drug Information
Pseudoephedrine | Wikipedia
Complete Pseudoephedrine (d-Isoephedrine) information from | Drugs.com
Pseudoephedrine for Stuffy Nose - Children's Hospital Colorado-Denver Area, Rocky Mountain Region