Tiludronic Acid; Uses, Dosage, Side Effects, Interactions, Pragnancy

Tiludronic acid is only found in individuals that have used or taken this drug. It is a bisphosphonate characterized by a (4-chlorophenylthio) group on the carbonation of the basic P-C-P structure common to all bisphosphonates. The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. < i> In vitro< /i> studies indicate that tiludronate acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable reduction in the enzymatic and transport processes that lead to resorption of the mineralized matrix. Bone resorption occurs following recruitment, activation, and polarization of osteoclasts. Tiludronate appears to inhibit osteoclasts by at least two mechanisms. disruption of the cytoskeletal ring structure, possibly by inhibition of protein-tyrosine-phosphatase, thus leading to detachment of osteoclasts from the bone surface and the inhibition of the osteoclastic proton pump.

Tiludronic acid is a bisphosphonate characterized by a (4-chlorophenylthio) group on the carbon atom of the basic P-C-P structure common to all bisphosphonates.

Mechanism of Action of Tiludronic acid 

The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. In vitro studies indicate that tiludronate acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable reduction in the enzymatic and transport processes that lead to resorption of the mineralized matrix. Bone resorption occurs following recruitment, activation, and polarization of osteoclasts. Tiludronate appears to inhibit osteoclasts by at least two mechanisms: disruption of the cytoskeletal ring structure, possibly by inhibition of protein-tyrosine-phosphatase, thus leading to detachment of osteoclasts from the bone surface and the inhibition of the osteoclastic proton pump. Non-nitrogenous bisphosphonates are metabolized by osteoclasts to compounds that then replace a portion of the adenosine triphosphate (ATP) molecule, making it non-functional. These non-functional molecules then competitively inhibit ATP in the cell, reducing cell energy and leading to apoptosis. Decreased levels of osteoclasts subsequently reduce the degree of breakdown of bone and bone turnover. Non-nitrogenous bisphosphonates are less potent relative to nitrogenous bisphosphonates.

Indications of Tiludronic acid 

• Prevention of osteoporosis
• Paget’s disease
• Treatment of osteoporosis in men to prevent fractures
• Treatment of osteoporosis in post-menopausal women to prevent fractures
• Treatment of osteoporosis in men to prevent fractures
• Prevention and treatment of corticosteroid-induced osteoporosis and prevention of bone loss in post-menopausal women considered at risk of developing osteoporosis.
• Prophylaxis and treatment of female osteoporosis
• Bone destruction
• Prevention and treatment of corticosteroid-associated osteoporosis together with supplements of calcium and vitamin D
• Treatment for osteogenesis imperfecta in patients of 18 years or older
• Dental implants coating (experimental)
• Treatment for osteogenesis imperfecta in patients of 18 years or older
• Dental implants coating (experimental)
• Osteoporosis caused by glucocorticoid
• For the treatment of Paget’s disease of bone (osteitis deformans).
• Indicated as an aid in the treatment of clinical signs of lameness associated with bone spavin in combination with a controlled exercise regime in horses over 3 years of age.

Contra-Indications of Tiludronic acid 

• Acute inflammations of the gastrointestinal tract (esophagitis, gastritis, ulcerations)
• Clinically manifest osteomalacia
• Certain malformations and malfunctions of the esophagus (strictures, achalasia)
• Inability to stand, walk, or sit for 30 minutes after oral administration
• Renal impairment with a creatinine clearance below 30ml/min
• Hypersensitivity to alendronate or another ingredient
• Hypocalcemia
• Pregnancy and breastfeeding
• Patients below 18 yrs. of age, as no clinical data exists
• Signs of colic, which is usually self-limiting, occurs in 30-45% of horses.
• Tachycardia
• Electrolyte disturbances – primarily calcium, magnesium, and potassium, which can last for several hours. Caution should be used in horses with disease processes that could be affected by electrolyte disturbances, such as hyperkalemic periodic paralysis or cardiac disease.
• Kidney damage – it is eliminated by the kidney and is not recommended for use in animals with impaired renal function.
• Less serious reactions include stiffness of the neck, decreased appetite, fever, and increased urination.

The dosage of Tiludronic acid

Side Effects of Tiludronic acid

The most common 

• Abdominal or stomach pain
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• Burning, itching, stinging, redness, or other sign of irritation at the application site ,rash
• Nausea
• painful or swollen gums
• numbness or heavy feeling in the jaw
• dull, aching pain in the hip, groin, or thigh
• liver problems,
• stomach pain,
• vomiting,
• Dizziness
• a headache,
• reversible hair loss or thinning, and
• fever.

Common

• chills or fever
• a headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in the chest
• discomfort in arms, shoulders, neck or upper back
• excessive sweating
• sudden drowsiness or need to sleep
• sharp pain when taking a deep breath
• coughing up blood
• rust colored urine
• liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
• decreased amount of urine

Rare

• Anxiety
• change in vision
• chest pain or tightness
• confusion
• a cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• a headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities
• severe pain in your upper stomach spreading to your back, nausea, and vomiting;
• signs of congestive heart failure–shortness of breath (even with mild exertion), cough with mucus, fast heartbeats, swelling, rapid weight gain, sleep problems;