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Ketorolac, also known as Ketorolac tromethamine, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat short-term moderate to severe pain. It belongs to the group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Ketorolac is not a narcotic and is not habit-forming. Ketorolac works by decreasing inflammation and pain. It is usually taken every 4 to 6 hours on a schedule or as needed for pain.

Uses

Ketorolac is used to relieve moderately severe pain, usually pain that occurs after an operation or other painful procedure. It is also used to treat pain from kidney stones, gout, and menstrual cramps. Ketorolac is not effective for the treatment of chronic pain, such as pain from arthritis.

Ketorolac is available in both oral and injectable forms. The oral form is taken by mouth, usually every 4 to 6 hours. The injectable form is given by a healthcare professional, usually every 6 to 8 hours.

Ketorolac is generally well-tolerated, but it can cause side effects such as stomach upset, nausea, vomiting, diarrhea, constipation, headache, dizziness, and drowsiness. Ketorolac can also increase the risk of bleeding, especially in people who are taking other blood thinners.

Ketorolac should not be used by people who are allergic to it, who have a history of stomach ulcers or bleeding, or who have severe kidney or liver disease. Ketorolac should also be used with caution in people who have heart disease, high blood pressure, or asthma.

If you are pregnant or breastfeeding, you should talk to your doctor before taking ketorolac. Ketorolac can pass into breast milk and may harm a nursing baby.

Ketorolac is a prescription drug. It is important to take ketorolac exactly as prescribed by your doctor. Do not take more ketorolac than prescribed, and do not take it for longer than prescribed. Taking too much ketorolac can increase the risk of side effects.

If you have any questions about ketorolac, talk to your doctor or pharmacist.

Dosage

The dosage of ketorolac will vary depending on the individual patient and the condition being treated. The usual recommended dose for adults is 10 mg every 4 to 6 hours as needed for pain. The maximum daily dose is 40 mg.

The dosage of ketorolac for children is based on body weight. The usual recommended dose for children is 0.5 mg/kg every 6 to 8 hours as needed for pain. The maximum daily dose is 1.5 mg/kg.

Ketorolac should not be used for more than 5 days in a row. If you need to take ketorolac for longer than 5 days, talk to your doctor.

If you have any questions about the dosage of ketorolac, talk to your doctor or pharmacist.

Administration

Ketorolac can be taken orally or by injection.

Oral administration⁚

Ketorolac tablets should be taken with a full glass of water.

Ketorolac tablets can be taken with or without food.

Do not crush or chew ketorolac tablets.

Injection administration⁚

Ketorolac injection is given by a healthcare professional.

Ketorolac injection is usually given into a muscle or vein.

Ketorolac injection can also be given into the space around the spinal cord.

General instructions⁚

Ketorolac should be taken exactly as prescribed by your doctor.

Do not take more ketorolac than prescribed.

Do not take ketorolac for longer than prescribed.

If you have any questions about how to take ketorolac, talk to your doctor or pharmacist.

Side Effects

Ketorolac can cause side effects, although not everyone gets them. Some of the most common side effects include⁚

Stomach upset

Nausea

Vomiting

Diarrhea

Constipation

Headache

Dizziness

Drowsiness

Ketorolac can also cause more serious side effects, such as⁚

Stomach ulcers

Bleeding from the stomach or intestines

Kidney damage

Liver damage

Heart attack

Stroke

If you experience any side effects from ketorolac, talk to your doctor or pharmacist.

The following are some tips to help reduce the risk of side effects from ketorolac⁚

Take ketorolac with food or milk to reduce stomach upset.

Avoid taking ketorolac for more than 5 days in a row.

Talk to your doctor if you have any stomach problems, kidney problems, or liver problems before taking ketorolac.

Tell your doctor about all the medications you are taking, including prescription drugs, over-the-counter drugs, and herbal supplements.

If you have any questions about the side effects of ketorolac, talk to your doctor or pharmacist.

Warnings and Precautions

Ketorolac should be used with caution in the following situations⁚

Stomach ulcers or bleeding⁚ Ketorolac can increase the risk of stomach ulcers and bleeding, especially in people who have a history of these conditions.

Kidney problems⁚ Ketorolac can worsen kidney function in people who have kidney problems.

Liver problems⁚ Ketorolac can worsen liver function in people who have liver problems.

Heart disease⁚ Ketorolac can increase the risk of heart attack and stroke in people who have heart disease.

Asthma⁚ Ketorolac can worsen asthma in people who have asthma.

Pregnancy⁚ Ketorolac should not be used during pregnancy.

Breastfeeding⁚ Ketorolac should not be used by breastfeeding mothers.

If you have any questions about the warnings and precautions associated with ketorolac, talk to your doctor or pharmacist.

The following are some tips to help reduce the risks associated with ketorolac⁚

Take ketorolac with food or milk to reduce stomach upset.

Avoid taking ketorolac for more than 5 days in a row.

Talk to your doctor if you have any stomach problems, kidney problems, or liver problems before taking ketorolac.

Tell your doctor about all the medications you are taking, including prescription drugs, over-the-counter drugs, and herbal supplements.

If you have any questions about the warnings and precautions associated with ketorolac, talk to your doctor or pharmacist.

Contraindications

Ketorolac is contraindicated in the following situations⁚

Allergic reaction⁚ Ketorolac should not be used by people who are allergic to it.

History of stomach ulcers or bleeding⁚ Ketorolac should not be used by people who have a history of stomach ulcers or bleeding.

Severe kidney disease⁚ Ketorolac should not be used by people who have severe kidney disease.

Severe liver disease⁚ Ketorolac should not be used by people who have severe liver disease.

Pregnancy⁚ Ketorolac should not be used during pregnancy.

Breastfeeding⁚ Ketorolac should not be used by breastfeeding mothers.

If you have any questions about the contraindications associated with ketorolac, talk to your doctor or pharmacist.

Drug Interactions

Ketorolac can interact with a number of other medications, including⁚

Anticoagulants⁚ Ketorolac can increase the risk of bleeding when taken with anticoagulants, such as warfarin.

Antiplatelet drugs⁚ Ketorolac can increase the risk of bleeding when taken with antiplatelet drugs, such as aspirin and clopidogrel.

Lithium⁚ Ketorolac can increase the levels of lithium in the blood, which can lead to lithium toxicity.

Methotrexate⁚ Ketorolac can increase the levels of methotrexate in the blood, which can lead to methotrexate toxicity.

Other NSAIDs⁚ Taking ketorolac with other NSAIDs can increase the risk of side effects, such as stomach ulcers and bleeding.

It is important to tell your doctor about all the medications you are taking, including prescription drugs, over-the-counter drugs, and herbal supplements. This will help your doctor to determine if ketorolac is safe for you to take.

If you have any questions about the drug interactions associated with ketorolac, talk to your doctor or pharmacist;

Overdose

An overdose of ketorolac can be dangerous and can lead to serious side effects, including⁚

Stomach bleeding

Kidney failure

Liver failure

Seizures

Coma

Death

If you think you have taken too much ketorolac, call your doctor or poison control center right away.

The symptoms of a ketorolac overdose can include⁚

Nausea

Vomiting

Diarrhea

Abdominal pain

Headache

Dizziness

Drowsiness

Confusion

Seizures

Coma

If you have any questions about the overdose of ketorolac, talk to your doctor or pharmacist.

Storage and Handling

Ketorolac should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). Ketorolac should be protected from light and moisture.

Ketorolac should not be stored in the bathroom or in other areas where it could be exposed to heat or moisture.

Ketorolac should be kept out of the reach of children.

If you have any questions about the storage and handling of ketorolac, talk to your doctor or pharmacist.

Pharmacology

Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID). NSAIDs work by inhibiting the production of prostaglandins, which are chemicals that cause inflammation and pain. Ketorolac is a potent NSAID and is effective in relieving moderate to severe pain.

Ketorolac is rapidly absorbed after oral administration and reaches peak plasma concentrations within 1 to 2 hours. The bioavailability of ketorolac is about 90%. Ketorolac is extensively bound to plasma proteins (99%).

Ketorolac is metabolized in the liver and excreted in the urine. The elimination half-life of ketorolac is about 5 to 6 hours.

Pharmacodynamics

Ketorolac is a non-selective inhibitor of cyclooxygenase (COX), the enzyme responsible for the synthesis of prostaglandins. Prostaglandins are lipids that play a role in inflammation, pain, and fever. By inhibiting COX, ketorolac reduces the production of prostaglandins, thereby reducing inflammation, pain, and fever.

Ketorolac has analgesic, anti-inflammatory, and antipyretic effects. It is a potent analgesic, with an efficacy comparable to that of morphine. Ketorolac is also a potent anti-inflammatory agent, with an efficacy comparable to that of indomethacin. Ketorolac has a moderate antipyretic effect.

Ketorolac has a rapid onset of action, with pain relief occurring within 30 minutes of oral administration. The duration of action of ketorolac is 4 to 6 hours.

Ketorolac is well-tolerated, with a low incidence of side effects. The most common side effects of ketorolac are gastrointestinal disturbances, such as nausea, vomiting, and diarrhea. Ketorolac can also cause dizziness, headache, and drowsiness.

Ketorolac is contraindicated in patients with a history of peptic ulcer disease, gastrointestinal bleeding, or hypersensitivity to ketorolac. Ketorolac should be used with caution in patients with renal impairment, hepatic impairment, or a history of asthma.

Pharmacokinetics

Ketorolac is rapidly and completely absorbed after oral administration, with peak plasma concentrations occurring within 30 to 60 minutes. The bioavailability of ketorolac is about 90%. Ketorolac is extensively bound to plasma proteins (99%).

Ketorolac is metabolized in the liver by cytochrome P450 enzymes, primarily CYP2C9. The major metabolites of ketorolac are inactive. Ketorolac is excreted in the urine, primarily as metabolites. The elimination half-life of ketorolac is about 5 to 6 hours.

The pharmacokinetics of ketorolac are linear over the dose range of 10 to 40 mg. Ketorolac does not accumulate in the body with repeated dosing.

Ketorolac is excreted in breast milk. The concentration of ketorolac in breast milk is about 1% of the maternal plasma concentration. Ketorolac should not be used by breastfeeding mothers.

Chemistry

Ketorolac is a non-steroidal anti-inflammatory drug (NSAID) that is used to relieve pain and inflammation. It is a white to off-white, crystalline powder with a slightly bitter taste. Ketorolac is soluble in water and alcohol.

The chemical name of ketorolac is (±)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. The molecular formula of ketorolac is C₁₅H₁₃NO₃. Ketorolac has a molecular weight of 255.27 g/mol.

Ketorolac is a racemic mixture of two enantiomers, (S)-ketorolac and (R)-ketorolac. The (S)-enantiomer is the more active enantiomer.

Ketorolac is synthesized by a multi-step process that starts with the reaction of benzoyl chloride and pyrrole. The resulting intermediate is then hydrogenated and cyclized to form ketorolac.

Ketorolac is a potent inhibitor of cyclooxygenase (COX), the enzyme responsible for the synthesis of prostaglandins. Prostaglandins are lipids that play a role in inflammation, pain, and fever. By inhibiting COX, ketorolac reduces the production of prostaglandins, thereby reducing inflammation, pain, and fever.

Ketorolac is a well-tolerated drug with a low incidence of side effects. The most common side effects of ketorolac are gastrointestinal disturbances, such as nausea, vomiting, and diarrhea. Ketorolac can also cause dizziness, headache, and drowsiness.

Stability

Ketorolac is a stable compound that is not affected by light or heat. Ketorolac solutions are stable for up to 24 hours at room temperature.

Ketorolac is compatible with the following diluents⁚

0.9% sodium chloride injection

5% dextrose injection

Lactated Ringer's injection

Ketorolac is not compatible with the following diluents⁚

Alkaline solutions

Solutions containing preservatives

Ketorolac should not be mixed with other drugs in the same syringe or IV bag.

Ketorolac should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). Ketorolac should be protected from light and moisture.

Ketorolac should not be stored in the bathroom or in other areas where it could be exposed to heat or moisture.

Ketorolac should be kept out of the reach of children.

Manufacturing

Ketorolac is a synthetic drug that is manufactured by a multi-step process. The starting material for the synthesis of ketorolac is benzoyl chloride. Benzoyl chloride is reacted with pyrrole to form an intermediate, which is then hydrogenated and cyclized to form ketorolac.

The synthesis of ketorolac is a complex process that requires specialized equipment and expertise. Ketorolac is manufactured in a cGMP-compliant facility that meets the highest standards of quality and safety.

The manufacturing process for ketorolac is closely monitored to ensure that the drug meets all of the required specifications. The drug is tested for purity, potency, and safety before it is released for sale.

Ketorolac is a safe and effective drug that is used to relieve pain and inflammation. The drug is manufactured in a cGMP-compliant facility that meets the highest standards of quality and safety.

The following are some of the key steps involved in the manufacturing process for ketorolac⁚

Reaction of benzoyl chloride and pyrrole⁚ Benzoyl chloride is reacted with pyrrole in a solvent to form an intermediate.

Hydrogenation of the intermediate⁚ The intermediate is hydrogenated in the presence of a catalyst to form a saturated intermediate.

Cyclization of the saturated intermediate⁚ The saturated intermediate is cyclized in the presence of a catalyst to form ketorolac.

Purification of ketorolac⁚ Ketorolac is purified by crystallization and recrystallization.

Drying and milling of ketorolac⁚ Ketorolac is dried and milled to a fine powder.

Packaging of ketorolac⁚ Ketorolac is packaged in vials or bottles.

The manufacturing process for ketorolac is a complex and carefully controlled process that ensures the production of a safe and effective drug.

Quality Control

Ketorolac is a prescription drug that is used to relieve pain and inflammation. It is important that ketorolac is manufactured to the highest standards of quality and safety.

The quality of ketorolac is controlled through a comprehensive quality control program that includes the following elements⁚

原料检验：所有用于制造凯托罗拉克的原料均经过严格的检验，以确保其符合规格。

In-process controls⁚ The manufacturing process for ketorolac is closely monitored to ensure that the drug meets all of the required specifications.

Finished product testing⁚ Each batch of ketorolac is tested for purity, potency, and safety before it is released for sale.

The quality control program for ketorolac is designed to ensure that the drug is safe and effective for use.

The following are some of the specific tests that are performed on ketorolac to ensure its quality⁚

Identity testing⁚ Ketorolac is tested to confirm its identity using a variety of analytical techniques, such as infrared spectroscopy and mass spectrometry.

Purity testing⁚ Ketorolac is tested for purity to ensure that it is free of impurities, such as other drugs or chemicals.

Potency testing⁚ Ketorolac is tested for potency to ensure that it contains the correct amount of active ingredient.

Safety testing⁚ Ketorolac is tested for safety to ensure that it does not cause any harmful side effects.

The quality control program for ketorolac is a comprehensive and rigorous program that ensures that the drug is safe and effective for use.

Regulatory Status

Ketorolac is a prescription drug that is regulated by the United States Food and Drug Administration (FDA). Ketorolac is approved for the short-term treatment of moderate to severe pain.

Ketorolac is available in both oral and injectable forms. The oral form of ketorolac is available in tablets and capsules. The injectable form of ketorolac is available in vials and syringes.

Ketorolac is a Schedule II controlled substance in the United States. This means that ketorolac has a high potential for abuse and addiction. Ketorolac can only be prescribed by a doctor and must be used according to the doctor's instructions.

Ketorolac is not approved for use in children under the age of 2 years. Ketorolac should be used with caution in elderly patients and patients with kidney or liver problems.

Ketorolac is a safe and effective drug when used as directed by a doctor. However, it is important to be aware of the potential risks and side effects of ketorolac before taking the drug.

The following are some of the regulatory requirements for ketorolac⁚

Ketorolac must be prescribed by a doctor.

Ketorolac must be used according to the doctor's instructions.

Ketorolac should not be used for more than 5 days in a row.

Ketorolac should not be used by people who are allergic to it.

Ketorolac should not be used by people who have a history of stomach ulcers or bleeding.

Ketorolac should not be used by people who have severe kidney or liver problems.

Ketorolac should be used with caution in elderly patients.

The regulatory requirements for ketorolac are designed to ensure the safe and effective use of the drug.

History

Ketorolac was first synthesized in 1973 by a team of scientists at Syntex Pharmaceuticals. The drug was initially developed as a non-steroidal anti-inflammatory drug (NSAID) with a long duration of action.

Ketorolac was approved for use in the United States in 1989. The drug was initially marketed under the brand name Toradol. Ketorolac is now available as a generic drug.

Ketorolac is a widely used NSAID for the treatment of moderate to severe pain. The drug is effective in relieving pain from a variety of sources, including surgery, trauma, and cancer.

Ketorolac is generally well-tolerated, but it can cause side effects such as stomach upset, nausea, vomiting, and diarrhea. Ketorolac can also increase the risk of bleeding, especially in people who are taking other blood thinners.

Ketorolac is a safe and effective drug when used as directed by a doctor. However, it is important to be aware of the potential risks and side effects of ketorolac before taking the drug.

The following are some of the key milestones in the history of ketorolac⁚

1973⁚ Ketorolac is first synthesized by a team of scientists at Syntex Pharmaceuticals.

1989⁚ Ketorolac is approved for use in the United States.

1990⁚ Ketorolac is marketed under the brand name Toradol.

2000⁚ Ketorolac becomes available as a generic drug.

Ketorolac is a valuable addition to the armamentarium of pain relievers. The drug is effective in relieving pain from a variety of sources and is generally well-tolerated.

Future Prospects

Ketorolac is a well-established and widely used NSAID for the treatment of moderate to severe pain. The drug is effective, well-tolerated, and has a long history of safe use.

However, there are some areas where ketorolac could be improved. For example, the drug can cause gastrointestinal side effects, such as stomach upset, nausea, and vomiting. Ketorolac can also increase the risk of bleeding, especially in people who are taking other blood thinners.

Researchers are working to develop new formulations of ketorolac that are less likely to cause these side effects. For example, one study found that a new formulation of ketorolac that was delivered in a liposomal formulation had a reduced risk of gastrointestinal side effects.

Another area where ketorolac could be improved is its duration of action. Ketorolac has a relatively short duration of action, and it must be taken multiple times per day to maintain pain relief. Researchers are working to develop new formulations of ketorolac that have a longer duration of action.

Overall, the future prospects for ketorolac are positive. The drug is a valuable addition to the armamentarium of pain relievers, and researchers are working to develop new formulations that are less likely to cause side effects and have a longer duration of action.

The following are some of the potential future developments for ketorolac⁚

New formulations with reduced side effects⁚ Researchers are working to develop new formulations of ketorolac that are less likely to cause gastrointestinal side effects and bleeding.

New formulations with a longer duration of action⁚ Researchers are working to develop new formulations of ketorolac that have a longer duration of action.

New uses for ketorolac⁚ Ketorolac is currently approved for the treatment of moderate to severe pain. Researchers are investigating new uses for ketorolac, such as the treatment of chronic pain and cancer pain.

Ketorolac is a valuable drug for the treatment of pain. Researchers are working to develop new formulations of ketorolac that are less likely to cause side effects and have a longer duration of action. These new formulations could make ketorolac an even more valuable tool for the treatment of pain.

Ketorolac

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