Pseudoephedrine

R01B - Nasal decongestants for systemic use ATC R01BA52 Small molecule approved 1963 Oral Natural product

JFDA label: Unifed Tablets

Mechanism of Action

Directly stimulates alpha-adrenergic receptors of respiratory mucosa causing vasoconstriction; directly stimulates beta-adrenergic receptors causing bronchial relaxation, increased heart rate and contractility

Indications

Approved

Nasal congestion

Contraindications

Source: Lexicomp

Concurrent administration with or within 2 weeks of discontinuing an MAO inhibitor Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (6)

Not Known Cardiac arrhythmia · chest tightness · circulatory shock (with hypotension) · hypertension · palpitations · tachycardia

Nervous system disorders (16)

Not Known Ataxia · central nervous system stimulation (transient) · chills · confusion · dizziness · drowsiness · excitability · fatigue · hallucination · headache · insomnia · nervousness · neuritis · restlessness · seizure · vertigo

Renal and urinary disorders (4)

Not Known Difficulty in micturition · dysuria · Polyuria · urinary retention

Blood and lymphatic system disorders (3)

Not Known Agranulocytosis · hemolytic anemia · thrombocytopenia

Immune system disorders (1)

Not Known Anaphylaxis

Gastrointestinal disorders (8)

Not Known Anorexia · constipation · diarrhea · dry throat · ischemic colitis · nausea · vomiting · xerostomia

Skin and subcutaneous tissue disorders (4)

Not Known Diaphoresis · skin photosensitivity · skin rash · urticaria

Musculoskeletal and connective tissue disorders (2)

Not Known Tremor · weakness

Eye disorders (2)

Not Known Blurred vision · diplopia

Ear and labyrinth disorders (1)

Not Known Tinnitus

Respiratory, thoracic and mediastinal disorders (6)

Not Known Dry nose · dyspnea · nasal congestion · pharyngeal edema · thickening of bronchial secretions · wheezing

Dosing

Source: Lexicomp

Nasal congestion: General dosing guidelines: Oral: Immediate release: 60 mg every 4 to 6 hours; Extended release: 120 mg every 12 hours or 240 mg every 24 hours; maximum: 240 mg per 24 hours

(For additional information see "Pseudoephedrine: Pediatric drug information") Nasal congestion: General dosing guidelines: Oral: Children: 4 to 5 years: 15 mg every 4 to 6 hours; maximum: 60 mg per 24 hours 6 to 11 years: 30 mg every 4 to 6 hours; maximum: 120 mg per 24 hours ≥12 years and Adolescents: Refer to adult dosing.

Nasal congestion: Use caution in this population; initiate using immediate release formulation: 30 to 60 mg every 6 hours as needed

There are no dosage adjustments provided in the manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Cardiovascular disease

Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease).

Diabetes

Use with caution in patients with diabetes mellitus.

Increased intraocular pressure/glaucoma

Use with caution in patients with increased intraocular pressure or angle-closure glaucoma.

Prostatic hyperplasia/urinary obstruction

Use with caution in patients with prostatic hyperplasia and/or GU obstruction.

Renal impairment

Use caution in patient with renal impairment; consider dosage adjustments.

Seizure disorder

Use with caution in patients with seizure disorder; may produce CNS stimulation.

Thyroid dysfunction

Use with caution in patients with thyroid dysfunction. Special populations:

Elderly

Use with caution in the elderly; may be more sensitive to adverse effects. Dosage form specific issues:

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.

Sodium

Some products may contain sodium. Other warnings/precautions:

Self-medication (OTC use)

When used for self-medication (OTC), notify healthcare provider if symptoms do not improve within 7 days or are accompanied by fever. Discontinue and contact healthcare provider if nervousness, dizziness, or sleeplessness occur. Not for OTC use in children

Pregnancy & Lactation

Pregnancy

Use of pseudoephedrine during the first trimester may be associated with a possible risk of gastroschisis, small intestinal atresia, and hemifacial microsomia due to pseudoephedrine's vasoconstrictive effects; additional studies are needed to define the magnitude of risk. Single doses of pseudoephedrine were not found to adversely affect the fetus during the third trimester of pregnancy (limited data); however, fetal tachycardia was noted in a case report following maternal use of an extended release product for multiple days. Decongestants are not the preferred agents for the treatment of rhinitis during pregnancy. Oral pseudoephedrine should be avoided during the first trimester.

Lactation

Pseudoephedrine is excreted into breast milk in concentrations that are ~4% of the weight adjusted maternal dose. The time to maximum milk concentration is ~1-2 hours after the maternal dose. Irritability has been reported in nursing infants (limited data; dose, duration, relationship to breast-feeding not provided). Milk production may be decreased in some women.

Chemistry & Properties

Formula	C10H15NO
Molecular weight	165.24 g/mol
IUPAC name	(1S,2S)-2-(methylamino)-1-phenylpropan-1-ol
CAS	90-82-4
PubChem CID	7028
InChIKey	`KWGRBVOPPLSCSI-WCBMZHEXSA-N`
logP	1.33 (XLogP 0.9)
Polar surface area	32.26 Å²
H-bond acceptors / donors	2 / 2
Drug-likeness (QED)	0.71
Lipinski violations	0

SMILES

CN[C@@H](C)[C@@H](O)c1ccccc1

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	10.0%
Half-life	4.412 h
Volume of distribution	3.128 L/kg
Protein binding	28.5%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP1A2	Substrate	—
CYP2C19	Substrate	—
CYP2D6	Inhibitor	—
CYP2D6	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Dihydroergotamine	major
Ergometrine	major
Ergotamine	major
Iobenguane (I-131)	major
Isocarboxazid	major
Linezolid	major
Methylene blue	major
Methylergometrine	major
Methysergide	major
Ozanimod	major
Phenelzine	major
Procarbazine	major
Selegiline	major
Tranylcypromine	major
Acarbose	moderate
Acebutolol	moderate
Acetohexamide	moderate
Albiglutide	moderate
Alfuzosin	moderate
Alogliptin	moderate
Amphetamine	moderate
Arformoterol	moderate
Atenolol	moderate
Atomoxetine	moderate
Benzphetamine	moderate
Betaxolol	moderate
Bisoprolol	moderate
Bromocriptine	moderate
Canagliflozin	moderate
Carvedilol	moderate
Chlorpropamide	moderate
Dapagliflozin	moderate
Deserpidine	moderate
Desvenlafaxine	moderate
Dexmethylphenidate	moderate
Dextroamphetamine	moderate
Diethylpropion	moderate
Digitoxin	moderate
Digoxin	moderate
Doxapram	moderate

Showing 40 of 100+.

Registered Products (45)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Tripofed	Suspension 1.25 mg/5 ml, 30 mg/5 ml	100 ml	Sun Set Drug Store	0.630
Trifed Expectorant	Suspension 100 mg/5 ml, 1.25 mg/5 ml, 30 mg/5 ml	100 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.650
Bronchofed Expectorant	Solution 30 mg, 100 mg, 1.25 mg	100 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	0.740
Trifed Expectorant	Suspension 30 mg/5 ml, 100 mg/5 ml, 1.25 mg/5 ml	120 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.750
Hatso Childrens cough	Suspension 100 mg/5 ml, 1 mg/5 ml, 15 mg/5 ml, 5 mg/5 ml	100 ml	Pharma International Company/ Jordan	0.800
Hatso Chlidrens Cold	Suspension 100 mg/5 ml, 1 mg/5 ml, 15 mg/5 ml	100 ml	Pharma International Company/ Jordan	0.800
Newfed	Suspension 1.25 mg/5 ml mg, 30 mg/5 ml mg	100 ml	Al-Gadeed Pharmaceutical Industries	0.810
Bronchofed Syrup	Syrup 30 mg, 1.25 mg	100 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	0.840
Trifed Syrup	Syrup 1.25 mg/5 ml, 30 mg/5 ml	100 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.840
PECTOLYN DECONGESTANT	Suspension 1.1 mg/5 ml, 57 mg/5 ml, 22.5 mg/5 ml, 14 mg/5 ml	150 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	0.850
Trifed PLUS Syrup	Syrup 125 mg/5 ml, 1.25 mg/5 ml, 25 mg/5 ml	100 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	0.880
Trifed Tablets	Tablet 2.5 mg, 60 mg	20 tab pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	0.890
SNIP TAB	Tablet 325 mg, 1 mg, 15 mg	20 tab pack varies	Al Hilal Drug Store	0.940
Rhinostop syrup	Syrup 100 mg/5 ml, Maleate 1 mg/5 ml, 20 mg/5 ml	100 ml	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	0.970
JOSWE NOCUF SYR	Syrup 100 mg/10 ml, 20 mg/10 ml, 5 mg/10 ml	120 ml	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	1.000
Unifed Tablets	Tablet 60 mg, 2.5 mg	20 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.040
Fludrex Syrup	Syrup 120 mg, 0.75 mg/5 ml, 15 mg	120 ml	Sun Set Drug Store	1.050
Unifed Expectorant Syrup	Syrup 100 mg/5 ml, 1.25 mg/5 ml, 30 mg/5 ml	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.050
Trifed Plus Tablets	Tablet 300 mg, 2.5 mg, 50 mg	20 tab	Hikma Pharmaceuticals Co.Ltd/Jordan	1.100
Unifed Syrup	Syrup 1.25 mg/5 ml, 30 mg/5 ml	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.210
Rhinostop tablet	Tablet 250 mg, Maleate 2.5 mg, 60 mg	20 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	1.250
Flutab Sinus 500mg/30mg	Tablet 500 mg, 30 mg	20 tab	Shawi & Rushedat Drug Store	1.270
Unifed DM Syrup	Syrup 30 mg/5 ml, 1.25 mg/5 ml, 10 mg/5 ml	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.370
SNIP TAB	Tablet 325 mg, 1 mg, 15 mg	30 tab pack varies	Al Hilal Drug Store	1.410
Unifed Extra Syrup	Syrup 50 mg, 1.25 mg, 10 mg, 7.5 mg	120 ml	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.440
Pamol Sinus	Tablet 500 mg, 30 mg	20 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	1.450
Revanin Sinus Caplets	Tablet 500 mg, 30 mg	20 Caplet	The Arab Pharmaceutical Manufactruing Co.	1.450
Revanin Cold & Flu Caplets	Tablet 500 mg, Maleate 2 mg, 30 mg	20 Caplet	The Arab Pharmaceutical Manufactruing Co.	1.520
Panda Sinus Double Strength	Tablet 1000 mg, 60 mg	12 tab	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	1.550
Ibugesic Cold & Sinus	Tablet 200 mg, 30 mg	20 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	1.590
Cetamol sinus	Tablet 575.0 mg, 30 mg	20 CAPLET/1 BOX	شركة الحياة للصناعات الدوائية / HAYAT PHARMA.INDUSTRIES.CO.LTD/JORDAN / Drug	1.720
Rhinostop tablet	Tablet 250 mg, Maleate 2.5 mg, 60 mg	30 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	1.880
Lemsip MAX Flu lemon	Tablet 1000 mg, 60 mg	10 tab	Nairoukh Drug Store	2.110
Rina-D 12 hours	Tablet 2.5 mg, 120 mg	10 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	2.140
Panadol Sinus Caplets	Tablet 500 mg, 30 mg	24 tab	Sukhtian Group	2.170
Panadol Cold & Flu	Tablet 500 mg, 2 mg, 30 mg	24 tab	Sukhtian Group	2.290
ADVIL COLD & SINUS CAPLET	Tablet 200 mg, 30 mg	20 Caplet	Sukhtian Group	2.370
Zeranase Tab	Tablet 120 mg, 5 mg	14 tab pack varies	The Arab Pharmaceutical Manufactruing Co.	3.390
CLARINASE Repetabs	Tablet 5 mg, 120 mg	14 tab	The Jordan Drugstore Co	3.670
Rina-D 12 hours	Tablet 2.5 mg, 120 mg	20 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	4.070
Zeranase Tab	Tablet 120 mg, 5 mg	20 tab pack varies	The Arab Pharmaceutical Manufactruing Co.	4.690
Rina-D 12 hours	Tablet 2.5 mg, 120 mg	30 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	6.030
Trifed Tablets	Tablet 2.5 mg, 60 mg	1000 tab pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	33.060
Unifed Tablets	Tablet 60 mg, 2.5 mg	1000 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	33.060
Rhinostop tablet	Tablet 250 mg, Maleate 2.5 mg, 60 mg	1000 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	53.130