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Opium: chemical constituents, therapeutic uses and commercial products
- 1. PHARMACOGNOSY AND PHYTOCHEMISTRY –II (BP504T) INSTITUTE OF PHARMACEUTICAL RESEARCH, GLA UNIVERSITY, MATHURA Module I: OPIUM Sonia Singh Assistant professor GLA University, Mathura
- 2. Objective of the class ■ Chemical constituents ■ Therapeutic uses ■ Commercial products Sonia Singh, Assistant Professor, GLA University, Mathura 2
- 3. Chemical constituents ■ Opium alkaloids usually occur naturally combined with a specific acid: (Meconic acid). ■ Meconic acid present only in Opium with morphine. ■ Meconic acid gives a deep purplish red-colored complex with FeCl3 ■ The latex contains mainly the alkaloids derived from amino acids phenylalanine and tyrosine. Meconic acid Sonia Singh, Assistant Professor, GLA University, Mathura 3
- 4. Classification of Opium alkaloids (1)Benzylisoquinoline alkaloids Eg: Papaverine, narcotine (2) Phenylethylamine alkaloids Eg: Narceine (3) Phenanthrene alkaloids Eg: Morphine, codeine, thebaine (4) Protopine Eg: Cryptopine Benzylisoquinoline Phenylethylamine PhenanthreneSonia Singh, Assistant Professor, GLA University, Mathura 4
- 5. Sonia Singh, Assistant Professor, GLA University, Mathura 5
- 6. ■ Fruits of poppy contain numerous off white coloured and minute seeds. ■ Seeds contain 30-35% drying fixed oil. ■ Commercially used in oil and paint industry. ■ Minor constituents: sugar, wax, mucilage, salts of calcium, potassium and magnesium. ■ Opium does not contain tannins, starch and calcium oxalate. Sonia Singh, Assistant Professor, GLA University, Mathura 6
- 7. Uses of Opium ■ As an analgesic. ■ Sleep-inducer (narcotic). ■ Treatment of coughs. Sonia Singh, Assistant Professor, GLA University, Mathura 7
- 8. Therapeutic uses ■ Papaverine :It has little or no analgesic or hypnotic properties put possesses spasmolytic and vasodilator activity. (antispasmodic for GIT spasms and in bronchial asthma). ■ Narcotine (Noscapine) :Anti-tussive and cough suppressant activity comparable to that of codeine, but no analgesic or narcotic action. Its original name ‘narcotine’ was changed to reflect this lack of narcotic action. ■ Morphine : Powerful analgesic and narcotic. It also induces a state of euphoria and mental detachment, together with nausea, vomiting, constipation, tolerance, and addiction. ■ Codeine: It produces morphine like analgesic effects. Always taken orally and is a component of many compound analgesic preparations. Relatively safe non-addictive medium analgesic. Anti-tussive action, helping to relieve and prevent coughing. ■ Thebaine: Devoid of analgesic activity. Its main value is as substrate for the semi- synthesis of other drugs Sonia Singh, Assistant Professor, GLA University, Mathura 8
- 9. Identification tests Morphine when sprinkled on nitric acid gives orange red colour. Codeine does not respond to this test. Morphine solution with potassium ferricyanide and ferric chloride solutions gives bluish green colour. Codeine does not respond to this test. Papaverine solutions in hydrochloric acid gives a lemon yellow colour with potassium ferricyanide solution. General test: Opium is dissolved in water and to the filtrate, ferric chloride solution is added by which deep reddish purple colour is obtained, which persists even on addition of hydrochloric acid. This indicates the presence of meconic acid. Sonia Singh, Assistant Professor, GLA University, Mathura 9
- 10. DRUG DRUG DESCRIPTION Codeine An opioid analgesic used to treat moderate to severe pain when the use of an opioid is indicated. Hydrocodone An opioid agonist used as an analgesic and antitussive agent. Ethylmorphine Ethylmorphine is an analgesic used for pain relief. Acetyldihydrocodeine Not Available Noscapine Investigated for use/treatment in lymphoma (non-hodgkin's), leukemia (lymphoid), cancer/tumors (unspecified), and multiple myeloma. Pholcodine Pholcodine is indicated as a cough suppressant for the temporary relief of non- productive dry cough. It is stated to present a required label indication of "temporary relief of dry cough."... Normethadone An opioid antitussive used to treat a cough associated with inflamed mucosa. Thebacon Not Annotated Dimemorfan Not Annotated Dextromethorphan An NMDA receptor antagonist used to treat cases of dry cough. Sonia Singh, Assistant Professor, GLA University, Mathura 10
- 11. ■ Alfentanil : Short-acting opioid analgesic . As an analgesic and in combination with general anaesthetics. Used in respiratory depressant in the management of mechanically ventilated patients under intensive care. ■ Fentanyl : 50 times more potent than morphine. ■ Levomethorphan: Narcotic analgesic 5-10 times potent as morphine and antitussive. ■ Dextromethorphan: Antitussive with no analgesic activity. Relief of non-productive cough. ■ Pentazocine: Both agonist and antagonist properties, good analgesic. ■ Dextropropoxyphene: Low analgesic activity, about half that of codeine, and finds application as a combination with aspirin or paracetamol. ■ Methadone: Treatment and rehabilitation of heroin addicts. Sonia Singh, Assistant Professor, GLA University, Mathura 11
- 12. ■ Some semi-synthetic derivatives of morphine : Codeine, Dihydrocodeine, Codeine, Dihydrocodeine, Pholcodine, Hydromorphone, Nalorphine ■ Some semi-synthetic derivatives of Thebaine : Naloxone, Naltrexone, Nalbuphine, Oxycodone, Etorphine Sonia Singh, Assistant Professor, GLA University, Mathura 12
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