The use and pharmacology of the chemical API loratadine powder

The chemical API, loratadine, is a second-generation antihistamine drug commonly used to treat allergy symptoms
.

It is used for allergic rhinitis, acute or chronic urticaria, allergic conjunctivitis, hay fever and other allergic skin diseases
.

Drug Name: Loratadine Foreign Name: Loratadine Alias: Ethyl Carboxylate Drug Type: Basic Pharmaceutical Chemical Formula: C22H23ClN2O2 Molecular Weight: 382.
883 Appearance: White or White-like Crystalline Powder CAS Login Number: 79794-75-5 Density: 1.
261 g/cm³ Melting Point: 134 to 136 °C Boiling Point: 531.
3 °C Flash Point: 275.
1 °C water-soluble: almost insoluble loratadine API CAS: 100643-71-8 regular GMP manufacturers pharmaceutical grade loratadine chemical API use: antihistamine, peripheral nerve H1 receptor has a high degree of selectivity, strong effect, long
time.

It is a long-acting tricyclic antihistamine that competitively inhibits histamine H1 receptors and inhibits allergic symptoms
caused by histamine.

There is no significant anticholine and central inhibitory effect
.

It is used to relieve symptoms related to allergic rhinitis, as well as to relieve symptoms
of chronic urticaria and other allergic skin diseases.

Pharmacology of pharmaceutical grade loratadine chemical API: piperidine antihistamines, derivatives of azatadine, have the effect
of selectively antagonizing peripheral histamine H1 receptors.

Its antihistamine action is fast, strong and long-lasting
.

Its effect is stronger
than that of astemizole and terfenadine.

This product has no sedative effect and no antimuscarinic choline effect
.

No strengthening effect
on ethanol.

Absorption is rapid and good
after oral administration.

The peak time of blood drug concentration tmax is 1.
5 hours
.

The binding rate to plasma proteins is 98%.


Most are metabolized in the liver, and the metabolite decarboxyethoxyloratadine still has antihistamine activity
.

This product and its metabolites are excreted from urine and feces, t1/2 is about 20 hours
.

This product and its metabolites are not easy to pass through the blood-brain barrier, but can appear in
breast milk.

Pharmacokinetics of pharmaceutical grade loratadine chemical APIs: well absorbed orally, rapidly and extensively metabolized in the liver, and eliminated by urine and
feces.

After taking the drug, the effect is fast, and some patients show the effect within 30 minutes, the tmax is 1.
5 to 2 h, and the elimination half-life is 8 to 14 h
.

The half-life of the active metabolite decarboxymethylethoxyloratadine (DCL) is 17 to 24 h
.

Half-lives may be longer
in the elderly and in patients with liver disease.

Loratadine has a binding rate of 97% to 99% to plasma proteins and a DCL rate of 73% to 76%.


After 24 hours of taking the drug, about 27% of the loratadine is excreted from the urine, after 10 days about 40% is eliminated from the urine, and 42% is excreted
from the stool.

With less milk secretion, so it is safe
to use the drug during lactation.

Indications for pharmaceutical grade loratadine chemical API: for allergic rhinitis, acute or chronic urticaria, allergic conjunctivitis, hay fever and other allergic skin diseases
.

Chlorratadine tablets made of pharmaceutical grade loratadine chemical APIs are also known as Karitan Brief introduction: [Properties] This product is a white tablet
.

【Specification】10 mg [Indications] is used to relieve symptoms related to allergic rhinitis, such as sneezing, runny nose, itchy nose, nasal congestion (nasal congestion is one of the common symptoms of otolaryngology, common causes include rhinitis, nasal septum deviation, nasal polyps, sinusitis, etc
.
).

Theoretically, nasal congestion can be resolved
by different treatments.

and itching and burning sensation in the
eyes.

Symptoms and signs of the nose and eyes are rapidly relieved by oral administration
.

It is also suitable for relieving the symptoms and signs
of chronic urticaria, pruritus skin diseases and other allergic skin diseases.

【Adverse reactions】 mainly include headache, drowsiness, fatigue, blurred mouth and vision, decreased or increased blood pressure, palpitations, syncope, hyperkinesia, liver function changes, jaundice, hepatitis, hepatic necrosis, hair loss, seizures, breast enlargement, erythema multiforme and generalized allergic reactions
.

【Drug interaction】1.
Simultaneous use of ketoconazole, macrolide antibiotics, cimetidin, theophylline and other drugs will increase the concentration of loratadine in plasma, and should be used with
caution.

Other drugs known to inhibit hepatic metabolism should be used with caution before interaction with loratadine is established
.

2.
Drugs that inhibit the function of liver drug metabolism enzymes can slow down
the metabolism of this product.

Taking ketoconazole 400 mg daily can increase the plasma concentration of loratadine and its active metabolite decarboxyethyl loratadine, but no ECG changes
have been observed.

Combined with macrolide antibiotics, cimetidine, theophylline and other drugs can also inhibit the metabolism
of loratadine.

3.
If you are taking other medicines, please consult a doctor or pharmacist
before using this product.

【Pharmacological effect】1.
This product is a high-efficiency, long-lasting tricyclic antihistamine, and a selective peripheral H1 receptor antagonist
.

May relieve various symptoms
caused by allergic reactions.

2.
Pharmacology This product is a long-acting tricyclic antihistamine, which inhibits the allergy symptoms
caused by histamine.

Loratadine tablets have no significant anticholine and central inhibitory effects
.

3.
Toxicological animal tests have not seen obvious teratogenic effects
.

Loratadine is an H1 receptor blocker, which is highly selective to peripheral H1 receptors and has a weak affinity for central H1 receptors, which can inhibit the release of leukotrienes and histamines
by mast cells.

This product has a fast onset of action, long-lasting effect, antihistamine effect is stronger than astepzole and terfenadine, and the antibian reaction effect is better
.

Loratadine API CDE filing can be checked with the goods peer quality inspection list