Oxycodone Hydrochloride

OXYCODONE HYDROCHLORIDE- oxycodone hydrochloride tablet
Rebel Distributors Corp

DESCRIPTION

Oxycodone Hydrochloride Tablets, USP are opioid analgesics.

Each tablet for oral administration contains 5 mg, 15 mg, or 30 mg of oxycodone hydrochloride USP.

Oxycodone hydrochloride is a white, odorless crystalline powder derived from the opium alkaloid, thebaine. Oxycodone hydrochloride dissolves in water (1 g in 6 to 7 mL) and is considered slightly soluble in alcohol (octanol water partition coefficient is 0.7).

Chemically, oxycodone hydrochloride is 4,5α-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one hydrochloride and has the following structural formula:

This is an image of the structural formula for oxycodone hydrochloride.
(click image for full-size original)

The tablets contain the following inactive ingredients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate, stearic acid. In addition, the 15 mg and 30 mg tablets contain FD&C Blue #1 aluminum lake, and the 15 mg tablets also contain D&C Yellow #10 aluminum lake.

The 5 mg, 15 mg, and 30 mg tablets contain the equivalent of 4.5 mg, 13.5 mg, and 27 mg, respectively, of oxycodone free base.

CLINICAL PHARMACOLOGY

Pharmacology:

The analgesic ingredient, oxycodone, is a semi-synthetic narcotic with multiple actions qualitatively similar to those of morphine; the most prominent of these involves the central nervous system and organs composed of smooth muscle.

Oxycodone, as the hydrochloride salt, is a pure agonist opioid whose principal therapeutic action is analgesia and has been in clinical use since 1917. Like all pure opioid agonists, there is no ceiling effect to analgesia, such as is seen with partial agonists or non-opioid analgesics. Based upon a single-dose, relative-potency study conducted in humans with cancer pain, 10 to 15 mg of oxycodone given intramuscularly produced an analgesic effect similar to 10 mg of morphine given intramuscularly. Both drugs have a 3 to 4 hour duration of action. Oxycodone retains approximately one half of its analgesic activity when administered orally.

Effects on Central Nervous System:

The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and play a role in the analgesic effects of this drug. A significant feature of opioid-induced analgesia is that it occurs without loss of consciousness. The relief of pain by morphine-like opioids is relatively selective, in that other sensory modalities, (e.g., touch, vibrations, vision, hearing, etc.) are not obtunded.

Oxycodone produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves both a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation.

Oxycodone depresses the cough reflex by direct effect on the cough center in the medulla. Antitussive effects may occur with doses lower than those usually required for analgesia. Oxycodone causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen due to hypoxia in overdose situations.

Effects on Gastrointestinal Tract and Other Smooth Muscle:

Oxycodone, like other opioid analgesics, produces some degree of nausea and vomiting which is caused by direct stimulation of the chemoreceptor trigger zone (CTZ) located in the medulla. The frequency and severity of emesis gradually diminishes with time.

Oxycodone may cause a decrease in the secretion of hydrochloric acid in the stomach that reduces motility while increasing the tone of the antrum, stomach, and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased to the point of spasm resulting in constipation. Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of sphincter of Oddi, and transient elevations in serum amylase.

Effects on Cardiovascular System:

Oxycodone, in therapeutic doses, produces peripheral vasodilatation (arteriolar and venous), decreased peripheral resistance, and inhibits baroreceptor reflexes. Manifestations of histamine release and/or peripheral vasodilatation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.

Caution should be used in hypovolemic patients, such as those suffering acute myocardial infarction, because oxycodone may cause or further aggravate their hypotension. Caution should also be used in patients with cor pulmonale who have received therapeutic doses of opioids.

Pharmacodynamics:

The relationship between the plasma level of oxycodone and the analgesic response will depend on the patient’s age, state of health, medical condition and extent of previous opioid treatment.

The minimum effective plasma concentration of oxycodone to achieve analgesia will vary widely among patients, especially among patients who have been previously treated with potent agonist opioids. Thus, patients need to be treated with individualized titration of dosage to the desired effect. The minimum effective analgesic concentration of oxycodone for any individual patient may increase with repeated dosing due to an increase in pain and/or development of tolerance.

Pharmacokinetics:

The activity of oxycodone hydrochloride tablets is primarily due to the parent drug oxycodone. Oxycodone hydrochloride tablets are designed to provide immediate release of oxycodone.

Table 1 Pharmacokinetic Parameters (Mean±SD)
Dose/ParametersAUC(ngxhr/mL)Cmax(ng/mL)Tmax(hr)Cmin(ng/mL)Cavg(ng/mL)Half-Life(hr)
Single Dose Pharmacokinetics
oxycodone hydrochloride tablets 5 mg tabs x 3133.2±3322.3±8.21.8±1.8n/an/a3.73±0.9
oxycodone hydrochloride tablets 15 mg tab128.2±35.122.2±7.61.4±0.7 n/an/a3.55±1.0
oxycodone hydrochloride oralconcentrate solution 15 mg oral solution130.6±34.721.1±6.11.9±1.5n/an/a3.71±0.8
oxycodone hydrochloride tablets 30 mg tab268.2±60.739.3±14.02.6±3.0n/a n/a3.85±1.3
Food-Effect, Single Dose
oxycodone hydrochloride oralsolution, USP 10 mg/10 mL oral sol’n (fasted)105±6.219.0±3.71.25±0.5n/an/a2.9±0.4
oxycodone hydrochloride oralsolution, USP 10 mg/10 mL oral sol’n (fed)133±25.217.7±3.02.54±1.2n/an/a 3.3±0.5

Multiple-Dose Studies

AUC(72-84)
oxycodone hydrochloride tablets 5 mg tabs q6h x 14 doses113.3±24.015.7±3.2 1.3±0.3 7.4±1.89.4±2.0 n/a
oxycodone hydrochloride oralsolution, USP 3.33 mg (3.33 mL) oral sol’n q4h x 21 doses99.0±24.812.9±3.11.0±0.37.2±2.3 9.7±2.6 n/a

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