Grastek tablets are derived from Timothy grass pollen. Grastek tablets are used sublingually to treat patients with allergic rhinitis and conjunctivitis (or without conjunctivitis) caused by an allergic reaction to grass pollen. The allergy is either confirmed by a positive skin test or in vitro testing by the development of IgE to Timothy grass or cross-reactive grass pollens.

Timothy grass pollen (Grastek Tablets) Uses:

• Grass pollen-induced allergic rhinitis:

  • Used as an immunotherapy for the treatment of allergic rhinitis-induced by grass pollen with or without conjunctivitis confirmed by positive skin test or in vitro testing for pollen-specific IgE antibodies for Timothy grass or cross-reactive grass pollens in patients of age ranging from 5 through 65 years. Not to be used for the immediate relief of allergy symptoms.

Timothy grass pollen (Grastek Tablets) Dose in Adults

Note:

• Dosage strength expressed in Bioequivalent Allergy Units (BAU). Note: The treatment should be started ≥12 weeks before the expected onset of each pollen season and continued throughout the pollen season.
• May take daily for 3 years consecutively (including intervals between grass pollen seasons). No Safety and efficacy have been established of initiating treatment during the ragweed pollen season.
• Limited data is available regarding restarting treatment after missing a dose; in clinical trials, treatment interruptions of ≤ one week were allowed.

Timothy grass pollen (Grastek Tablets) Dose in the treatment of Grass pollen-induced allergic rhinitis:

• Adults ≤65 years:

  • Sublingual: 1 tablet (2,800 BAU) once a day

Timothy grass pollen (Grastek Tablets) Dose in Childrens

Note:

• Dosage strength expressed in Bioequivalent Allergy Units (BAU). The treatment should be started ≥12 weeks before the expected onset of each pollen season and continued throughout the pollen season.
• May take daily for 3 years consecutively (including intervals between grass pollen seasons). No Safety and efficacy have been established of initiating treatment during the ragweed pollen season.
• Limited data is available regarding restarting treatment after missing a dose; in clinical trials, treatment interruptions of ≤ one week were allowed.

Timothy grass pollen (Grastek Tablets) Dose in the treatment of Grass pollen-induced allergic rhinitis:

• Children ≥5 years and Adolescents:

  • Sublingual: One tablet (2,800 BAU) once a day. Administer the 1st dose in a health care setting as there is a potential for allergic reactions.

Pregnancy Risk Factor B

• Animal reproduction studies have not shown any adverse effects.

Use during breastfeeding:

• It is unknown if breast milk contains grass pollen allergen extract.
• Follow the manufacturer's instructions. Nursing women should be treated with caution

Dose in Kidney Disease:

No dosage adjustments provided in the manufacturer’s labeling.

Dose in Liver disease:

No dosage adjustments provided in the manufacturer’s labeling.

Common Side Effects of Timothy grass pollen (Grastek Tablets):

• Dermatologic:

  • Pruritus of ear

• Gastrointestinal:

  • Oral itching

• Hypersensitivity:

  • Mouth edema

• Respiratory:

  • Throat irritation

Less Common Side Effects of Timothy grass pollen:

• Cardiovascular:

  • Chest Discomfort
  • Lip Edema

• Central Nervous System:

  • Headache
  • Oral Hypoesthesia
  • Fatigue

• Dermatologic:

  • Tongue Pruritus
  • Lip Pruritus
  • Pruritus
  • Urticaria

• Endocrine & Metabolic:

  • Palatal Edema

• Gastrointestinal:

  • Oral Paresthesia
  • Lip Swelling
  • Oral Mucosa Erythema
  • Swollen Tongue
  • Dyspepsia
  • Nausea
  • Oral Discomfort
  • Dysphagia
  • Glossalgia
  • Glossitis
  • Stomatitis
  • Tongue Disease
  • Abdominal Pain
  • Gastroesophageal Reflux Disease

• Ophthalmic:

  • Eye Pruritus

• Respiratory:

  • Pharyngeal Erythema
  • Oropharyngeal Pain
  • Cough
  • Pharyngeal Edema
  • Dry Throat
  • Nasal Congestion
  • Nasal Discomfort
  • Sneezing
  • Dyspnea
  • Constriction Of The Pharynx

Contraindications to Timothy grass pollen (Grastek Tablets):

• Hypersensitivity to any inactive ingredients (mannitol or gelatin) in this product, or any other component of its formulation.
• Asthma (severe or unstable asthma)
• Any history of severe allergic reactions or severe local reactions to sublingual allergen immunotherapy
• An earlier history of eosinophilic esophagitis

Canadian labeling: Additional contraindications not in US labeling

• FEV1 70% (unstable, severe, chronic, or severe seasonal asthma)
• Combination therapy with beta-blockers
• Oral inflammation (eg, oral lichen planus, oral ulcerations, severe oral candidiasis, or dental extraction).

Warnings and precautions

• Esophagitis:

  • Eosinophilic reflux may be caused by sublingual tablet immunotherapy. 
  • Patients with persistent or severe gastroesophageal symptoms (eg dysphagia, chest discomfort) should stop receiving therapy.
  • Therapy is not recommended for patients with eosinophilic esophagitis.

• Hypersensitivity reactions: [US Boxed Warning]

  • This could lead to life-threatening allergic reactions including anaphylaxis or severe laryngopharyngeal restrictions.
  • Local reactions may occur in the throat or mouth. Patients who experience persistent and escalating adverse reactions to the mouth or throat should be advised not to use this medication.
  • Concomitant use of allergen immunotherapy may increase the risk for systemic or local adverse reactions.

• Respiratory disease: [US-Boxed Warning]

  • Patients with severe, unstable or uncontrolled asthma should not be given this medication. There are no studies on patients with moderate and severe asthma.
  • Do not treat acute asthma exacerbations.
  • Recurrent asthma exacerbations should be evaluated and the patient should be re-evaluated.
  • Recurrent asthma exacerbations should be considered when considering treatment discontinuation.
  • The contraindication to the use of asthma medication is uncontrolled or unstable asthma.

Monitoring parameters:

• Signs/symptoms of hypersensitivity
• Monitoring should be done for at least 30 minutes after giving the 1st dose.

How to administer Timothy grass pollen (Grastek Tablets)?

Sublingual:

• The 1st dose should be given in a healthcare setting as there is a potential for allergic reactions; monitoring should be done for at least 30 minutes after giving the 1st dose & may give subsequent doses at home if well tolerated by the patient.
• With dry hands, the sublingual tablet may be removed from the blister immediately before administration.
• The tablet should be placed under the tongue until completely dissolved and then wait at least 1 minute before swallowing.
• Must wash hands after handling the tablet. The food or beverage should be avoided for 5 minutes following administration.
• Make auto-injectable epinephrine available to patients

Mechanism of action of Timothy grass pollen (Grastek Tablets):

• The grass pollen allergen extract includes an extract from timothygrass. 
• Although the mechanism of action is still unclear, it has been suggested that specific immunotherapy (SIT), may induce a switch between T helper 2 and T helper 1 cells (Th2) responses.
• This results in a decrease of interleukin-4 and interleukin-5, respectively, and an increase in interleukin-10, (IL-10). IgG-blocking antibody production that competes with IgE antibodies for allergen-binding, proliferation of regulatory T lymphocytes, cytokines and eosinophils, as well as a decrease in mast cells and eosinophils.

International Brand Names of Timothy grass pollen:

• Grastek

Timothy grass pollen Brand Names in Pakistan:

No Brands Available in Pakistan.