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What is the expected pharmacological action of morphine?

What is the expected pharmacological action of morphine?

This medication is used to help relieve moderate to severe pain. Morphine belongs to a class of drugs known as opioid analgesics. It works in the brain to change how your body feels and responds to pain.

Why is morphine administered slowly?

Morphine must be injected slowly; rapid intravenous administration may result in chest wall rigidity. Inspect Morphine Sulfate Injection for particulate matter and discoloration prior to administration.

How is morphine absorbed into the body?

Absorption. Morphine is absorbed into the bloodstream via multiple routes of administration including: Orally in the form of tablets or capsules. Rectally inside suppositories or gel-coated capsules that can be inserted into the anus so the drug can be absorbed into the rectal blood vessels.

What is the best way to administer morphine?

Morphine injection comes as a solution (liquid) to inject intramuscularly (into a muscle) or intravenously (into a vein). It is usually injected once every 4 hours as needed. Use morphine injection at around the same times every day.

How is IV morphine metabolized?

The metabolism of morphine. Regardless of the mode of administration, approximately 44–55% of a morphine dose is converted to M3G, 9–10% to M6G, and 8–10% is excreted in the urine unchanged. 8, 12 Four percent of a morphine dose is excreted as normorphine and its glucuronide metabolites.

What is the pharmacokinetics of morphine sulphate?

Excretion: After an oral dose, about 60% is excreted in the urine in 24 hours, with about 3% excreted as free morphine in 48 hours. After a parental dose, about 90% is excreted in 24 hours, with about 10% as free morphine, 65 to 70% as conjugated morphine, 1% as normorphine and 3% as normorphine glucuronide.

How fast is morphine absorbed?

Morphine is modestly absorbed from the gastrointestinal tract following oral administration. Following oral administration of radiolabelled morphine to humans, peak plasma levels were reached after approximately 15 minutes.

Is IV morphine metabolized in the liver?

Morphine is metabolized by the liver to morphine-6-glucuronide (active metabolite) and morphine-3-glucuronide (inactive metabolite with potential neurotoxic effects), which are then cleared renally.

How does the body metabolise morphine?

Morphine is primarily metabolized in the liver by uridine-5′-diphosphate (UDP) glucoronosyltransferase, with specific affinity for the UGT2B7 isoenzyme. This isoenzyme is responsible for the formation of both glucuronide species, but at different amounts (5 times more M3G than M6G).

What is the bioavailability of morphine?

Absolute bioavailability for morphine was estimated to be 23.9% after oral solution, 22.4% after MST-Continus and 18.7% after the buccal tablet. Maximum plasma morphine concentrations were seen at 45 min (oral solution), 2.5 h (MST) and 6 h (buccal).

How is morphine transported in the body?

Morphine crosses the blood-brain barrier easier than M6G but M6G can be actively transported by Oatp2 and by de novo synthesis of M6G from mor- phine in the brain. Those mechanisms together make it possible that M6G is the main analgesic, responsible for up to 97% of morphine analgesic effect.

What is the bioavailability of morphine for an intravenous injection?

Morphine administered intravenously (8.8 mg) and by inhalation (17.6 mg) produced approximately the same maximal degree of ventilatory depression. This finding is consistent with the bioavailability value of 59%. Fig.

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