| Drug Index |
| GENERIC NAME : |
| heroin |
| BRAND NAMES : |
| none in the United States. In the United Kingdom it is available by prescription as diamorphine and in The Netherlands as diacetylmorphine for long-term heroin addicts. |
| STREET NAMES : |
| China white, fix, horse, smack, whack, mother pearl, H. junk, black tar, skag, |
| BRIEF DESCRIPTION : |
| Heroin is an opiate (narcotic) that binds to the mu-opiate receptor. It is an opioid agonist. It is considered a central nervous system depressant and slows the action of smooth muscle. As with other opiates, heroin is used both as a pain-killer (but not legally in the United States) and a recreational drug.
One of the most common methods of heroin use is via intravenous injection (typically known as "shooting up"). If taken orally, heroin undergoes extensive first-pass metabolism via deacetylation, making it a prodrug (A prodrug is a pharmacological substance (drug) that is administered in one form for conversion in the body to another form called the active metabolite). Heroin is converted in the body to the active metabolite morphine when taken orally (by mouth). When the drug is injected, however, it avoids this first-pass effect, very rapidly crossing the blood-brain barrier due to the presence of the acetyl groups, which render it much more lipid-soluble than morphine itself. Once in the brain, it is deacetylated into 3- and 6-monoacetylmorphine and morphine, which bind to mu-opioid receptors resulting in intense euphoria (“high”), decreased pain perception, and anxiolytic effects (relief of anxiety). Examples of other powerful opioid agonists include hydromorphone, methadone, morphine, oxycodone, and fentanyl.
The primary source worldwide is from certain species of the poppy plant. The opium poppy was cultivated in lower Mesopotamia as long ago as 3400 BC. The chemical analysis of opium in the 19th century revealed that most of its activity could be ascribed to two ingredients, codeine and morphine. Heroin was first synthesized in 1874 by C.R. Alder Wright, an English chemist working at St. Mary's Hospital Medical School in London, England. He had been experimenting with combining morphine with various acids. He boiled anhydrous morphine alkaloid with acetic anhydride over a stove for several hours and produced a more potent, acetylated form of morphine, now called diacetylmorphine. From 1898 through to 1910 heroin was marketed as a non-addictive morphine substitute and cough suppressant. Bayer marketed heroin as a cure for morphine addiction before it was discovered that heroin is rapidly metabolized into morphine, and as such, heroin was basically only another form of morphine. The company was embarrassed by this new finding and it became a historical blunder for Bayer. In the United States the Harrison Narcotics Tax Act was passed in 1914 to control the sale and distribution of heroin and other opiates. The law did allow heroin to be prescribed and sold for medical purposes. In particular, recreational users could often still be legally supplied with heroin and use it. In 1924, the United States Congress passed additional legislation banning the sale, importation or manufacture of heroin in the United States. It is now a Schedule I substance, and is thus illegal in the United States. |
| INDICATIONS FOR USE : |
| Heroin is not legal in most countries. It is considered a "street" drug in most countries that is abused for the euphoric effect ("high") and sedating effect. It is a powerful analgesic (pain killer). However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom, and in The Netherlands, heroin is available for prescription as the generic drug diacetylmorfine for treatment of long-term heroin addiction. |
| ABUSE AND ADDICTIVE POTENTIAL : |
Use of heroin poses an extremely high for abuse or dependence. Heroin is used as a recreational drug for the profound relaxation and intense euphoria ("high") it produces, although the effect diminishes with increased tolerance (requiring larger or more frequent dosages of heroin to produce relief of pain or achieve a state of euphoria). A symptom that is easily detected with opiate use is pinpoint pupils (miosis). Signs of withdrawal can occur in some individuals after using heroin less than a week consecutively. Addiction to this drug almost always occurs when used for several weeks consecutively. Once an individual has become dependent on heroin, a primary driving force to continue using heroin (or substituting other opiate agonists) is to prevent the very unpleasant neurochemical and physical withdrawal syndrome associated with discontinuing this drug. Symptoms usually associated with withdrawal may include: • Abdominal pain • Muscle aches • Joint pain • Sleep problems (insomnia) • Agitation, Restlessness • Diarrhea • Dilated pupils • Goose bumps • Nausea • Runny nose • Sweating • Vomiting • Restlessness • Yawning • Loss of appetite (anorexia) • Rapid heart rate • Elevated blood pressure • Rapid breathing • Eyes or nose watering Withdrawal of heroin is best handled by a physician that is skilled at assisting patients with opiate detoxification. Medications are often necessary to help control symptoms of withdrawal. |
| OVERDOSAGE : |
| Acute overdose of herion can cause respiratory depression, extreme drowsiness or prolonged sleeping, stupor or coma, muscle flaccidity, cold/clammy skin, constricted pupils, slow heart rate (bradycardia), low blood pressure (hypotension), and death. When heroin is used in combination with alcohol or other central nervous system depressants, the two drugs potentiate one another and can greatly enhance the risk for overdose. Because of the dangers associated with overdose, immediate medical attention should be sought. |
| CAUTIONS : |
| Any patient with a history of alcohol or substance dependence has a very high risk for developing addiction to heroin. Respiratory depression is the chief hazard from all opioid agonist medications. Serious medical problems can occur in individuals with impaired lung function or low blood pressure. There may be serious problems also with use of this medication an individual with a closed head injury. It can elevate cerebrospinal fluid pressure and mask symptoms of closed head injury that could require immediate medical measures. It may obscure the diagnosis or clinical course in individuals with acute abdominal conditions. Individuals with kidney (renal) or liver (hepatic) impairment are at great risk of higher levels in the bloodstream than individuals with normal kidney or liver function. Use of heroin with other sedative/hypnotic drugs, opiates (narcotics), muscle relaxers, sedating "street drugs", or alcohol can cause a multiplied effect of the potency of each drug (called potentiation). Taking these types of drugs with heroin is considered dangerous. There are also other prescription medications that may interact negatively with oxymorphone heroin. Also, since it is primarily bought "off the street" there is no way to know what amount or potency of heroin is present in the "substance" that is obtained from a non-pharmaceutical source. Also, heroin is often "cut" (diluted) with fillers (such as sugar, starch, or powdered milk) or cheaper drugs (some of which may be dangerous themselves, and especially when combined with heroin as they may potentiate one another). Because one never knows the actual strength of heroin purchased off the street, users are at risk for overdose or death. Heroin also poses a risk of spread of HIV or Hepatitis B by sharing needles. |
| SIDE EFFECTS : |
| Side effects of heroin use may include nausea, constipation, abdominal cramping, vomiting, headache, and pruritus (itching), hypotension (low blood pressure). Adverse effects may include allergic reaction, irregular heartbeat, migraine, confusion, temporary hallucination, dry mouth, nervousness, tremor, rash, blurred vision, mental clouding, lethargy, mood changes, urinary retention, anxiety, fear, respiratory depression, and personality changes. |
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