Loratadine

R06A - Antihistamines for systemic use ATC R06AX13 Small molecule approved 1993 Oral Prodrug Natural product

Active form: Desloratadine.

JFDA label: Ramitin 10mg tablet

Mechanism of Action

Antagonist of Histamine H1 receptor — Histamine H1 receptor antagonist

Target	Action	Gene / class
Histamine H1 receptor efficacy	ANTAGONIST	HRH1

Indications

Approved

Allergic rhinitis
Urticaria

Contraindications

Source: Lexicomp

Hypersensitivity to loratadine or any component of the formulation Absolute

Adverse Reactions

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

Nervous system disorders (7)

Common Drowsiness · fatigue · Headache · malaise · nervousness · Somnolence (low rate vs older AH) · voice disorder

Gastrointestinal disorders (5)

Common abdominal pain · Dry mouth · stomatitis · Xerostomia

Uncommon Nausea

Skin and subcutaneous tissue disorders (2)

Common Skin rash

Rare Allergic skin reactions (paradoxical)

Musculoskeletal and connective tissue disorders (1)

Common Hyperkinesia

Eye disorders (1)

Common Conjunctivitis

Infections and infestations (1)

Common Viral infection

General disorders and administration site conditions (1)

Common Fatigue

Other (1)

Very Common Central nervous system: Headache

Respiratory, thoracic and mediastinal disorders (5)

Common epistaxis · flu-like symptoms · pharyngitis · upper respiratory tract infection · Wheezing

Dosing

Source: Lexicomp

Seasonal allergic rhinitis, urticaria: Oral: 10 mg daily once daily or 5 mg twice daily (RediTabs)

(For additional information see "Loratadine: Pediatric drug information") Children 2-5 years: Seasonal allergic rhinitis, urticaria: Oral: 5 mg once daily Children ≥6 years: Refer to adult dosing.

Refer to adult dosing.

No dosage adjustment provided in manufacturer’s labeling; however, the following recommendations have been recommended (Aronoff, 2007): Adults: CrCl 10-50 mL/minute: Recommended dose every 24 to 48 hours. CrCl Dialysis: Recommended dose every 48 hours. Continuous renal replacement therapy (CRRT): No dosage adjustment necessary if clearance is 2000 mL/minute. Children ≥2 years: No dosage adjustment necessary for any degree of renal impairment.

No dosage adjustment provided in manufacturer’s labeling; however, hepatic impairment increases systemic exposure to loratadine.

Warnings & Precautions

Source: Lexicomp

Hepatic impairment

Hepatic impairment increases systemic exposure. Use with caution.

Renal impairment

Use with caution in patients with renal impairment. Concurrent drug therapy issues:

Sedatives

Effects may be potentiated when used with other sedative drugs or ethanol. 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.

Phenylalanine

Some products may contain phenylalanine.

Pregnancy & Lactation

Pregnancy

FDA category B

Safe

First-line antihistamine for rhinitis/urticaria in pregnancy. Extensive safety data

Lactation

RID 1.1%

Loratadine and its active metabolite, desloratadine, are present in breast milk. The relative infant dose (RID) of loratadine plus desloratadine has been calculated to be 1.1% when compared to a maternal dose of 40 mg/day of loratadine (Hilbert 1988). In general, breastfeeding is considered acceptable when the RID is 25% breastfeeding should generally be avoided (Anderson 2016; Ito 2000). The estimated daily infant dose of loratadine equivalents via breast milk was calculated to be 29.1 mcg/da

Chemistry & Properties

Formula	C22H23ClN2O2
Molecular weight	382.89 g/mol
IUPAC name	ethyl 4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidine-1-carboxylate
CAS	79794-75-5
PubChem CID	3957
InChIKey	`JCCNYMKQOSZNPW-UHFFFAOYSA-N`
logP	4.89 (XLogP 5.2)
Polar surface area	42.43 Å²
H-bond acceptors / donors	3 / 0
Drug-likeness (QED)	0.70
Lipinski violations	0

SMILES

CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB -0.3)

Enzyme interactions

Enzyme	Role	Detail
CYP2B6	Inhibitor	—
CYP2B6	Substrate	—
CYP2C19	Inhibitor	IC₅₀ 0.21166010488516734 µM
CYP2C19	Substrate	—
CYP2C8	Inhibitor	IC₅₀ 2.95 µM
CYP2C9	Inhibitor	—
CYP2C9	Substrate	—
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Receptor binding (top 3)

Target	Action	Affinity
H1 receptor (HRH1)	Antagonist	pKi 7.4
TRPV2 (TRPV2)	Channel blocker	pIC50 5.5
B0AT2 (SLC6A15)	Inhibitor	pIC50 5.4

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)OCT1 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)P-gp (Substrate)

Drug–drug interactions (78, DDInter)

Interacting drug	Severity	Management
Abametapir (topical)	moderate
Amiodarone	moderate
Apalutamide	moderate
Boceprevir	moderate
Bosentan	moderate
Brigatinib	moderate
Candida albicans	moderate
Celecoxib	moderate
Coccidioides immitis spherule	moderate
Conivaptan	moderate
Dalfopristin	moderate
Darunavir	moderate
Dasatinib	moderate
Deferasirox	moderate
Diltiazem	moderate
Dronedarone	moderate
Duvelisib	moderate
Echinacea	moderate
Efavirenz	moderate
Enzalutamide	moderate
Etravirine	moderate
Fedratinib	moderate
Fluvoxamine	moderate
Fosnetupitant	moderate
Fostamatinib	moderate
Glycerol phenylbutyrate	moderate
Grepafloxacin	moderate
Histamine	moderate
Idelalisib	moderate
Imatinib	moderate
Iodide I-123	moderate
Iodide I-131	moderate
Isavuconazonium	moderate
Ivacaftor	moderate
Larotrectinib	moderate
Lefamulin	moderate
Letermovir	moderate
Lonafarnib	moderate
Lorlatinib	moderate
Lumefantrine	moderate

Showing 40 of 78.

Registered Products (43)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Lostamin	Suspension 5 mg/5 ml	100 ml	Al Saleem Drug Store	0.790
Klarihist Syrup	Syrup 5 mg/5 ml	60 ml pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.680
Lohist	Suspension 5 mg/5 ml	100 ml	Reda Jardaneh Drug Store	1.710
Lorine Syrup	Syrup 5 mg/5 ml	100 ml	Shawi & Rushedat Drug Store	2.060
Restamine Tablets	Tablet 10 mg	10 tab pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	2.060
Clara	Tablet 10 mg	10 tab	شركة مستودع ادوية الايمان	2.120
Lorine Tab	Tablet 10 mg	10 tab pack varies	Shawi & Rushedat Drug Store	2.120
Lohist	Tablet 10 mg	10 tab pack varies	Reda Jardaneh Drug Store	2.220
Klarihist tablets	Tablet 10 mg	10 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	2.430
Lorax	Tablet 10 mg	10 tab	Sukhtian Group	2.430
Histal Tablet	Tablet 10 mg	10 tab pack varies	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	2.450
Lorax	Injection 1 mg/ml	120 ml	Sukhtian Group	2.470
Tidilor syrup	Syrup 1 mg/1 ml	100 ml	Pharma International Company/ Jordan	2.490
LORATAN TABLETS	Tablet 10 mg	10 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	2.500
Ramitin	Tablet 10 mg	10 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	2.500
Tidilor tab	Tablet 10 mg	10 tab pack varies	Pharma International Company/ Jordan	2.500
Loreen Tablet	Tablet 10 mg	10 tab pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	2.540
Lormine Syrup	Syrup 0.1 % w/v	100 ml	PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN	2.540
Ramitin-5mg syrup	Syrup 5 mg/5 ml	100 ml	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	2.730
Loratan Syrup	Syrup 5 mg/5 ml	100 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	2.790
HISTAL SYR	Syrup 5 mg/5 ml	100 ml pack varies	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	2.800
Klarihist Syrup	Syrup 5 mg/5 ml	100 ml pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	2.800
Loreen Syrup	Syrup 5 mg/5 ml	100 ml pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	2.860
Clara Syrup	Syrup 5 mg/5 ml	100 ml	شركة مستودع ادوية الايمان	2.980
Loreen Syrup	Syrup 5 mg/5 ml	125 ml pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	3.150
HISTAL SYR	Syrup 5 mg/5 ml	120 ml pack varies	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	3.360
CLARITINE Syrup	Syrup 1 mg/ml	120 ml	The Jordan Drugstore Co	3.530
CLARINASE Repetabs	Tablet 5 mg, 120 mg	14 tab	The Jordan Drugstore Co	3.670
LORATAN TABLETS	Tablet 10 mg	20 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	3.700
Lorine Tab	Tablet 10 mg	20 tab pack varies	Shawi & Rushedat Drug Store	4.030
Lohist	Tablet 10 mg	20 tab pack varies	Reda Jardaneh Drug Store	4.220
Klarihist tablets	Tablet 10 mg	20 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	4.620
Ramitin	Tablet 10 mg	20 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	4.750
Klarihist tablets	Tablet 10 mg	30 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	6.850
Ramitin	Tablet 10 mg	30 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	7.130
Tidilor tab	Tablet 10 mg	30 tab pack varies	Pharma International Company/ Jordan	7.130
CLARITINE Tablets	Tablet 10 mg	30 tab	The Jordan Drugstore Co	8.580
Histal Tablet	Tablet 10 mg	250 tab pack varies	JORDAN SWEDEN MEDICAL&STERILE.CO(JOSWE)/JORDAN	50.230
LORATAN TABLETS	Tablet 10 mg	400 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	85.000
Tidilor tab	Tablet 10 mg	500 tab pack varies	Pharma International Company/ Jordan	103.390
Loreen Tablet	Tablet 10 mg	600 tab pack varies	Hayat Pharmaceutical Industries CO.PLC/JORDAN	129.540
Restamine Tablets	Tablet 10 mg	1000 tab pack varies	Hikma Pharmaceuticals Co.Ltd/Jordan	165.470
Ramitin	Tablet 10 mg	1000 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	212.500