Opioids
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Opioids
Opium and its derivatives, commonly known as opiates, are drugs that depress the central nervous system, reducing physical sensation and the ability to respond to stimuli. It is derived from the opium poppy and has been recognized for at least 2,000 years to have pain-relieving and euphoria-inducing qualities. It comes under the classification of depressant drugs.
It is derived from the opium poppy and has been recognized for at least 2,000 years to have pain-relieving and euphoria-inducing qualities. It comes under the classification of depressant drugs.
Difference between Opioids and Opiates
- OPIOIDS: a generic term applied to alkaloids from the opium poppy, their synthetic analogs, and compounds synthesized in the body.
- OPIATES: a subset of opioids comprising the various products derived from the opium poppy Including opium, morphine, and heroin.
Mechanism
Opiate medicines all bind to the same brain chemicals called opiate receptors. The potency of these medications is determined by how soon they reach the receptors and how much energy it takes to activate them. Opiates affect the brain’s neuroreceptor sites in extremely particular ways. It mirrors the action of endorphins, the nervous system’s natural painkillers, and is highly addictive.
The rate at which opiates enter the body is determined by the method of administration. Opioids reach peak levels in the brain within minutes after being smoked or injected. The faster this happens, the greater the risk of overdosing and death. Because drugs must pass through the mucous membranes of the nose to reach the blood vessels beneath, they are absorbed more slowly when snorted.
Repeated opioid use decreases endorphin production, requiring more opium to occupy the vacant opioid receptors and alleviate pain. When the medicine wears off, there is no longer any protection against pain, resulting in the intense withdrawal symptoms linked with these drugs.
Drug Action
The stimulation of opiate receptors produces analgesia, euphoria, miosis(contraction of the pupil of the eye), hypotension, bradycardia(slow heartbeat), and respiratory depression Opioid receptors fall into different types, each of which has subtypes. The main types are µ, κ 𝑎𝑛𝑑 δ receptors.
| µ (Mu) | Analgesia, Euphoria, Miosis, Sedation, Constipation, Respiratory Depression, Hormonal changes, Cough suppression, Nausea |
| κ (kappa) | Analgesia, Diuresis(excessive production of urine), Sedation, Dysphoria, Hallucination, Respiratory depression |
| δ (Delta) | Analgesia, Convulsant (producing sudden and involuntary muscle contractions) |
The µ receptor is essential for the development of opioid dependence. The µ receptor is potassium channel-linked and inhibits adenylate cyclase. The binding of morphine to the µ receptors inhibits the release of GABA from the nerve terminals, reducing the inhibitory effect of GABA on the dopaminergic neurons. The increased activation of dopaminergic neurons in the nucleus accumbens and the ventral tegmental areas that are part of the brain’s reward pathway and the release of dopamine into the synaptic result in sustained activation of the postsynaptic membrane. Continued activation of the dopaminergic reward pathway leads to feelings of euphoria.
As a result of these discoveries, medicines that modulate opioid receptors have been developed. Categories of medicines are:
- Agonists bind to opioid receptors to provide a pleasurable feeling and so lessen the desire for opiates, but they have fewer psychological and physiological side effects than opiates.
- Partial agonist Maximum effect is less than a full agonist (e.g., buprenorphine)
- Antagonists bind to opioid receptors in the same way that agonists do, but they don’t activate them; instead, they ‘block’ the receptors so that opiates can’t access them. Antagonists don’t give you a good feeling and don’t satisfy your appetite.
Types of Opioids
Morphine
It was discovered by German pharmacist Friedrich Sertürner between 1803 and 1805. This is thought to be the first time an active component from a plant has been isolated and therefore Morphine, the new form, was acclaimed as “God’s own medicine”. It is made by dissolving opium in acid and neutralizing it with ammonia. It is used to treat severe pain, but only at very small dosages and for very short periods.
How is it Taken?
It could be taken orally in the form of tablets or through injections.
- Codeine: The sap of the opium poppy, Papaver somniferum, contains codeine naturally. It is most commonly used to relieve mild to moderate pain.
HOW IS IT TAKEN?
Commonly used as a prescription drug, codeine is given by medical prescription for cough, pain, and diarrhea. It is available as a tablet, a capsule, and a solution (liquid) to consume by mouth (alone or in combination with other drugs). It’s commonly taken every 4 to 6 hours, depending on the situation.
- Semi-synthetic opioids: These are derived from the chemicals in opium. Eg, Hydromorphone, Oxycodone, Heroin, Buprenorphine
- Heroin: Heroin is an opioid manufactured from morphine, a natural chemical extracted from the seed pods of several opium poppy plants grown in Southeast and Southwest Asia, Mexico, and Colombia. Heroin can come in the form of a white or brown powder, as well as a black sticky material is known as black tar heroin.
HOW IS IT TAKEN?
People use heroin through injecting, sniffing, snorting, or smoking it. It can be smoked or chased by heating on tin foil and inhaling the sublimate. Speedballing is a practice in which people mix heroin and crack cocaine. It is commonly known by different names including Brown sugar, Chiva Dope, Horse, Junk, Skag, Skunk, Smack, and White Horse.
EFFECTS
Short-term effects of heroin include euphoria; dry mouth; itching; nausea; vomiting; analgesia; slowed breathing and heart rate. If the person is using the drug for long enough, then they are likely to experience its long-term effects that include Collapsed veins; abscesses(swollen tissue with pus); infection of the lining and valves in the heart; constipation and stomach cramps; liver or kidney disease; and pneumonia.
- Buprenorphine: Buprenorphine is a partial opioid agonist. At low to moderate doses, it causes feelings of euphoria or respiratory depression. These effects are weaker with buprenorphine than with complete opioid agonists like methadone and heroin. Buprenorphine is both safe and effective when taken as directed.
Synthetic opioids chemicals are created in a lab and act on the same brain receptors as natural opioids.
- Fentanyl: Fentanyl is a strong synthetic opioid that is 50 to 100 times more potent than morphine. It is a prescribed medicine that is also illegally manufactured and utilised. It’s a drug that’s similar to morphine in that it’s used to treat people who are in a lot of pain, especially after surgery. It’s also used to treat chronic pain in patients who are physically tolerant of other opioids.
HOW IS IT TAKEN?
Fentanyl can be given as a shot, a patch that is applied to the skin, or lozenges that are sucked like cough drops when prescribed by a doctor. Synthetic fentanyl is sold illegally as a powder, blotter paper, eye droppers, nasal sprays, and pills that resemble other prescription opioids.
EFFECTS
The effects of fentanyl include extreme happiness, drowsiness, nausea, confusion, constipation, sedation, problem breathing, and unconsciousness.
- Methadone: Methadone is the most well-known agonist medication for treating heroin addiction. It is addictive in and of itself, although it causes less psychological harm and has fewer physical side effects than heroin. It inhibits heroin cravings and minimises withdrawal symptoms when taken orally in modest dosages as Methadone when taken orally enters the bloodstream and then the brain gradually, preventing the “rush” feeling. The withdrawal symptoms are likewise gradual because it is absorbed slowly.
Commonly Abused Synthetic Opioids in India
- Tidigesic/buprigesic/lupigesic (IV or IM) Buprenorphine
- Tramazac/Ultracet (Oral) Tramadol
- Lomotil (Oral) Diphenoxylate
- Fortwin (IM or IV) Pentazocine
- Spasmo Proxyvon (SP) oral or IV Dextropropoxyphene(+ Paracetamol + Dicyclomine) – banned in India
- Spasmo Proxyvon plus: Tramadol (+ Paracetamol + Dicyclomine)
Local Formulations in India
- Bhooki is a cigarette rolled with poppy husk seeds.
- Doda– Dry straw grounded to powder and mixed with water and filter it through a piece of cloth several times. The tea-coloured liquid, which is odourless and tasteless, is then drunk by the glassfuls.
- Poppy tea decoction made of poppy straw.
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