| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| ln Vivo |
For the treatment of allergic rhinitis and chronic urticaria, avastin (usually 8 mg three times daily) is an efficient and well-tolerated antihistamine. Treating seasonal allergic rhinitis with Avastin is more successful than using a placebo and works similarly to clemastine or terfenadine. Akvastine works similarly to commonly used doses of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine, or terfenadine in the treatment of dermatoses in which histamine plays a causative role. It is also more effective than a placebo. Compared to clemastine, avastin is less drowsy, and its side effect profile is similar to that of terfenadine or placebo [1]. Avastin at doses of 4 mg and 8 mg significantly reduced symptoms of seasonal allergic rhinitis, including scores for runny nose, sneezing, and overall scores. Furthermore, the symptom scores for watery eyes and scratchy throat were decreased by 8 mg of acrivastine. When treating seasonal allergic rhinitis, avastin is well tolerated and works well [2].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Acrivastine was absorbed rapidly from the combination capsule following oral administration and was as bioavailable as a solution of acrivastine. After administration of SEMPREX-D Capsules, maximum plasma acrivastine concentrations were achieved at 1.14 ± 0.23 hour. A mass balance study in 7 healthy volunteers showed that acrivastine is primarily eliminated by the kidneys. Over a 72-hour collection period, about 84% of the administered total radioactivity was recovered in urine and about 13% in feces, for a combined recovery of about 97%. 0.46 ± 0.05 L/kg 2.9 ± 0.7 mL/min/kg Biological Half-Life The mean terminal half-life for acrivastine was 1.9 ± 0.3 hours following single oral doses and increased to 3.5 ± 1.9 hours at steady state. The terminal half-life for the propionic acid metabolite was 3.8 ± 1.4 hours. |
| Toxicity/Toxicokinetics |
Hepatotoxicity
Acrivastine has not been linked to liver enzyme elevations or to instances of clinically apparent liver injury. Its relative safety may relate to its rapid metabolism and use in low dosages. Likelihood score: E (unlikely cause of clinically apparent liver injury). References on the safety and potential hepatotoxicity of antihistamines are given together after the Overview section on Antihistamines. Drug Class: Antihistamines Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Small occasional doses of acrivastine would not be expected to cause any adverse effects in breastfed infants. Larger doses or more prolonged use may cause drowsiness and other effects in the infant or decrease the milk supply, particularly in combination with a sympathomimetic such as pseudoephedrine or before lactation is well established. The nonsedating antihistamines are preferred alternatives. ◉ Effects in Breastfed Infants Relevant published information on acrivastine was not found as of the revision date. In one telephone follow-up study, mothers reported irritability and colicky symptoms 10% of infants exposed to various antihistamines and drowsiness was reported in 1.6% of infants. None of the reactions required medical attention. ◉ Effects on Lactation and Breastmilk Antihistamines in relatively high doses given by injection can decrease basal serum prolactin in nonlactating women and in early postpartum women. However, suckling-induced prolactin secretion is not affected by antihistamine pretreatment of postpartum mothers. Whether lower oral doses of antihistamines have the same effect on serum prolactin or whether the effects on prolactin have any consequences on breastfeeding success have not been studied. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. Protein Binding Acrivastine binding to human plasma proteins was 50 ± 2.0%. |
| References |
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| Additional Infomation |
Acrivastine is a member of the class of pyridines that is (pyridin-2-yl)acrylic acid substituted at position 6 by a [(1E)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl group. It is a non-sedating antihistamine used for treatment of hayfever, urticaria, and rhinitis. It has a role as a H1-receptor antagonist. It is an alpha,beta-unsaturated monocarboxylic acid, a member of pyridines, a N-alkylpyrrolidine and an olefinic compound.
Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia. Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D. Acrivastine is a Histamine-1 Receptor Antagonist. The mechanism of action of acrivastine is as a Histamine H1 Receptor Antagonist. Acrivastine is a second generation antihistamine that is used for the treatment of allergic rhinitis. Acrivastine has not been linked to instances of clinically apparent acute liver injury. Acrivastine is a synthetic alkylamine with non-sedative antihistaminergic activity. Acrivastine competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of gastrointestinal smooth muscle, caused by actions of histamine on bronchial, and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes. (NCI05) Drug Indication For the relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. FDA Label |
| Molecular Formula |
C22H24N2O2
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| Molecular Weight |
348.4382
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| Exact Mass |
348.183
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| CAS # |
87848-99-5
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| Related CAS # |
Acrivastine-d7;172165-56-9
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| PubChem CID |
5284514
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
555.1±50.0 °C at 760 mmHg
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| Melting Point |
55.5-59.5 °C(lit.)
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| Flash Point |
289.5±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
4.55
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
514
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC(C)=CC=1)(\C1C=CC=C(/C=C/C(=O)O)N=1)=C/CN1CCCC1
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| InChi Key |
PWACSDKDOHSSQD-IUTFFREVSA-N
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| InChi Code |
InChI=1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+
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| Chemical Name |
(E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~143.50 mM)
H2O : ~1 mg/mL (~2.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8699 mL | 14.3497 mL | 28.6993 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01732510 | TERMINATEDWITH RESULTS | Drug: MK-8226 Drug: Placebo |
Atopic Dermatitis | Merck Sharp & Dohme LLC | 2012-12-21 | Phase 1 |
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