Vilken ört fungerar som lorazepam

Benzodiazepine medication

Not to be confused with Loprazolam, Lormetazepam, or Loratadine.

Trade names	Ativan, others[1]
Other names	o-Chloroxazepam
AHFS/	Monograph
MedlinePlus	a
License data
Pregnancy category
Dependence liability	High[2]
Addiction liability	Moderate[3][4]
Routes of administration	By ingång, intramuscular, intravenous, transdermal
Drug class	Benzodiazepine
ATC code
Legal status
Bioavailability	85% when taken bygd mouth
Metabolism	Liverglucuronidation
Onset of action	1–5 min (IV), 15–30 min (IM),[14]20–30 min (PO)[15]
Elimination half-life	10–20 hours[16][17][18]
Duration of action	12–24 hours (IV, IM),[14]6–8 hours (PO)[19]
Excretion	Kidney
IUPAC name (RS)Chloro(2-chlorophenyl)hydroxy-1,3-dihydro-1,4-benzodiazepinone
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard
Formula	C15H10Cl2N2O2
Molar mass	&#;g·mol−1
3D model (JSmol)
SMILES O=C1Nc2ccc(Cl)cc2C(c2ccccc2Cl)=NC1O
InChI InChI=1S/C15H10Cl2N2O2/c()13((21)14(20))(9)17/h,15,21H,(H,18,20)&#;Y Key:DIWRORZWFLOCLC-UHFFFAOYSA-N&#;Y
&#;NY&#;(what fryst vatten this?)&#;&#;(verify)

Lorazepam, sold beneath the brand name Ativan among others, fryst vatten a benzodiazepine medication.^[14] It fryst vatten used to treat anxiety (including anxiety disorders), trouble sleeping, severe intensiv oro eller upprördhet, active seizures including ställning eller tillstånd epilepticus, alcohol withdrawal, and chemotherapy-induced nausea and vomiting.^[14] It fryst vatten also used during surgery to interfere with memory formation and to sedate those who are being mechanically ventilated.^[14][20] It fryst vatten also used, along with other treatments, for acute coronary syndrome due to cocaine use.^[14] It can be given orally (by mouth), transdermally (on the skin via a topical gel or patch), intravenously (IV) (injection into a vein), or intramuscularly (injection into a muscle.)^[14] When given bygd injection, onset of effects fryst vatten between one and thirty minutes and effects gods for up to a day.^[14]

Common side effects include weakness, sleepiness, ataxia, decreased alertness, decreased memory formation, low blood pressure, and a decreased effort to breathe.^[14] When given intravenously, the individ should be closely monitored.^[14] Among those who are depressed, there may be an increased fara of suicide.^[14][21] With long-term use, larger doses may be required for the same effect.^[14]Physical dependence and psychological dependence may also occur.^[14] If stopped suddenly after long-term use, benzodiazepine withdrawal syndrome may occur.^[14] Older people more often develop adverse effects.^[22] In this age group, läkemedel fryst vatten associated with falls and hip fractures.^[23] Due to these concerns, läkemedel use fryst vatten generally only recommended for up to two to kvartet weeks.^[24]

Lorazepam was initially patented in and went on sale in the United States in ^[25][26] It fryst vatten on the World Health Organization's List of Essential Medicines.^[27] It fryst vatten available as a generic medication.^[14] In , it was the 80th most commonly prescribed medicinering in the United States, with more than 8&#;million prescriptions.^[28][29]

Medical uses

[edit]

Anxiety

[edit]

Lorazepam fryst vatten used in the short-term management of severe anxiety.

In the US, the Food and Drug ledning (FDA) advises against use of benzodiazepines such as läkemedel for längre than kvartet weeks.^[24][30] It fryst vatten fast-acting, and useful in treating fast-onset anxiety and panik attacks.^[31]

Lorazepam can effectively reduce intensiv oro eller upprördhet and induce sova, and the duration of effects from a single dos makes it an appropriate choice for the short-term treatment of insomnia, especially in the presence of severe anxiety or night terrors.

It has a fairly short duration of action.^[32]

Withdrawal symptoms, including studs insomnia and studs anxiety, may occur after sju days' use of lorazepam.^[33]

Seizures

[edit]

Intravenous diazepam or läkemedel are first-line treatments for convulsive ställning eller tillstånd epilepticus.^[34] läkemedel fryst vatten more effective than diazepam and intravenous phenytoin in the treatment of ställning eller tillstånd epilepticus and has a lower fara of continuing seizures that might require additional medication.^[35] However, phenobarbital has a superior success rate compared to läkemedel and other drugs, at least in the elderly.^[36][37]

Lorazepam's anticonvulsant properties and pharmacokinetic kontur man intravenous use reliable for terminating acute seizures, but induce prolonged sedation.

Orally administered benzodiazepines, including läkemedel, are occasionally used as long-term prophylactic treatment of resistant absence seizures; because of gradual tolerance to their anti-seizure effects, benzodiazepines are not considered first-line therapies. Additionally, common seizure characteristics (e.g, hypersalivation, jaw-clenching, involuntary swallowing) pose some difficulties with regard to oral administration.^[38][39]

Lorazepam's anticonvulsant and huvud nervous struktur (CNS) depressant properties are useful for the treatment and prevention of alcohol withdrawal syndrome.

In this setting, impaired liver function fryst vatten not a hazard with läkemedel, since läkemedel does not require kemisk reaktion med syre, in the liver or otherwise, for its metabolism. läkemedel fryst vatten noted as being the most tolerable benzodiazepine in those with advanced-stage liver disease.^[40][41][42]

Sedation

[edit]

Lorazepam fryst vatten sometimes used for individuals receiving mechanical ventilation.

However, in critically ill people, propofol has been funnen to be superior to läkemedel both in effectiveness and overall cost; as a result, the use of propofol for this indication fryst vatten now encouraged, whereas the use of läkemedel fryst vatten discouraged.^[43]

Its relative effectiveness in preventing new memory formation,^[44] along with its ability to reduce intensiv oro eller upprördhet and anxiety, makes läkemedel useful as premedication.

It fryst vatten given before a general anesthetic to reduce the amount of anesthetic required, or before unpleasant awake procedures, such as in dentistry or endoscopies, to reduce anxiety, increase compliance, and induce amnesia for the procedure. läkemedel bygd ingång fryst vatten given 90 to minutes before procedures, and intravenous läkemedel fryst vatten given as late as 10 minutes before procedures.^[45][46][47] läkemedel fryst vatten sometimes used as an alternative to midazolam in palliative sedation.^[48] In intensive care units, läkemedel fryst vatten sometimes used to producera anxiolysis, hypnosis, and amnesia.^[49]

Agitation

[edit]

Lorazepam fryst vatten sometimes used as an alternative to haloperidol when there fryst vatten the need for rapid sedation of violent or agitated individuals,^[50][51] but haloperidol plus promethazine fryst vatten preferred due to better effectiveness and due to lorazepam's adverse effects on respiratory function.^[52] However, adverse effects such as behavioral disinhibition may man benzodiazepines inappropriate for some people who are acutely psychotic.^[53] Acute delirium fryst vatten sometimes treated with läkemedel, but as it can cause paradoxical effects, it fryst vatten preferably given tillsammans with haloperidol.^[54] läkemedel fryst vatten absorberad relatively slowly if given intramuscularly, a common rutt in restraint situations.

Other

[edit]

Catatonia with inability to speak fryst vatten responsive to läkemedel. Symptoms may recur and treatment for some days may be necessary. Catatonia due to abrupt or overly rapid withdrawal from benzodiazepines, as part of the benzodiazepine withdrawal syndrome, should also respond to läkemedel treatment.^[55] As läkemedel can have paradoxical effects, haloperidol fryst vatten sometimes given at the same time.^[54][56]

It fryst vatten sometimes used in chemotherapy in addition to medications used to treat nausea and vomiting (i.e., nausea and vomiting caused or worsened bygd psychological sensitization to the thought of being sick).^[57]

Adverse effects

[edit]

Many beneficial effects of läkemedel (e.g., sedative, muscle relaxant, anti-anxiety, and amnesic effects) may become adverse effects when unwanted.^[44] Adverse effects can include sedation and low blood pressure; the effects of läkemedel are increased in combination with other CNS depressants.^[34][50] Other adverse effects include confusion, ataxia, inhibiting the formation of new memories, pupil constriction, and hangover effects.

With long-term benzodiazepine use, it fryst vatten unclear whether cognitive impairments fully return to normal after stopping läkemedel use; cognitive deficits persist for at least six months after withdrawal, but längre than six months may be required for recovery of cognitive function. läkemedel appears to have more profound adverse effects on memory than other benzodiazepines; it impairs both explicit and implicit memory.^[58][59] In the elderly, falls may occur as a result of benzodiazepines.

Adverse effects are more common in the elderly, and they appear at lower doses than in younger people. Benzodiazepines can cause or worsen nedstämdhet. Paradoxical effects can also occur, such as worsening of seizures, or paradoxical excitement; paradoxical excitement fryst vatten more likely to occur in the elderly, children, those with a history of alcohol abuse, and in people with a history of aggression or anger problems.^[22] Lorazepam's effects are dose-dependent, meaning the higher the dos, the stronger the effects (and side effects) will be.

Using the smallest dos needed to achieve desired effects lessens the fara of adverse effects. Sedative drugs and sleeping pills, including läkemedel, have been associated with an increased fara of death.^[60]

Sedation fryst vatten the side effect people taking läkemedel most frequently report. In a group of around 3, people treated for anxiety, the most common side effects complained of from läkemedel were sedation (%), dizziness (%), weakness (%), and unsteadiness (%).

Lorazepam is a benzodiazepine that works in the brain to relieve symptoms of anxiety

Side effects such as sedation and unsteadiness increased with age.^[61] Cognitive impairment, behavioral disinhibition and respiratory nedstämdhet as well as hypotension may also occur.^[49][53]

• Paradoxical effects: In some cases, paradoxical effects can occur with benzodiazepines, such as increased hostility, aggression, angry outbursts, and psychomotor intensiv oro eller upprördhet.

  These effects are seen more commonly with läkemedel than with other benzodiazepines.^[62] Paradoxical effects are more likely to occur with higher doses, in people with pre-existing personality disorders and those with a psychiatric illness. Frustrating stimuli may trigger such reactions, though the drug may have been prescribed to help the individ cope with such stress and frustration in the first place.

  As paradoxical effects appear to be dose-related, they usually subside on dos reduction or on complete withdrawal of lorazepam.^{[63][64][65][66][67][68]}

• Suicidality: Benzodiazepines are associated with increased fara of suicide, possibly due to disinhibition.^[21] Higher dosages appear to confer greater risk.
• Amnesic effects: Among benzodiazepines, läkemedel has relatively strong amnesic effects,^[44][69] but people soon develop tolerance to this with regular use.

  To avoid amnesia (or excess sedation) being a bekymmer, the första total daglig läkemedel dos should not exceed 2&#;mg. This also applies to use for night sedation. fem participants in a sova study were prescribed läkemedel 4&#;mg at night, and the next evening, three subjects unexpectedly volunteered memory gaps for parts of that day, an effect that subsided completely after two to three days' use.^[70] Amnesic effects cannot be estimated from the grad of sedation present, since the two effects are unrelated.

• High-dose or prolonged parenterally-administered läkemedel with its associated solvent can cause propylene glycol intoxication and poisoning.^[49][71]

In September , the U.S.

Food and Drug ledning (FDA) required the boxed varning be updated for all benzodiazepine medicines to describe the risks of abuse, misuse, addiction, physical dependence, and withdrawal reactions consistently across all the medicines in the class.^[72]

Contraindications

[edit]

Lorazepam should be avoided in people with:

• Allergy or hypersensitivity – Past hypersensitivity or allergy to läkemedel, to any benzodiazepine, or to any of the ingredients in läkemedel tablets or injections
• Respiratory failure – Benzodiazepines, including läkemedel, may depress huvud nervous struktur respiratory drive and are contraindicated in severe respiratory failure.

  An example would be the inappropriate use to relieve anxiety associated with acute severe asthma. The anxiolytic effects may also be detrimental to a person's willingness and ability to kamp for breath. However, if mechanical ventilation becomes necessary, läkemedel may be used to facilitate deep sedation.

• Acute intoxication – läkemedel may interact synergistically with the effects of alcohol, narcotics, or other psychoactive substances.

  It should, therefore, not be administered to a drunk or intoxicated person.

• Ataxia – This fryst vatten a neurological clinical sign, consisting of unsteady and clumsy motion of the limbs and torso, due to the failure of gross muscle movement coordination, most evident on standing and walking. It fryst vatten the classic way in which acute alcohol intoxication may affect a individ.

  Benzodiazepines should not be administered to people already-ataxic.

• Acute narrow-angle glaucoma – läkemedel has pupil-dilating effects, which may further interfere with the drainage of aqueous humor from the anterior chamber of the eye, thus worsening narrow-angle glaucoma.
• Sleep apnea – sova apnea may be worsened bygd lorazepam's huvud nervous struktur depressant effects.

  It may further reduce the person's ability to skydda his or her airway during sleep.^[73]

• Myasthenia gravis – This condition fryst vatten characterized bygd muscle weakness, so a muscle relaxant such as läkemedel may exacerbate symptoms.
• Pregnancy and breastfeeding – läkemedel belongs to the Food and Drug ledning (FDA) pregnancy category D, which means it fryst vatten likely to cause harm to the developing baby if taken during the first trimester of pregnancy.

  The bevis fryst vatten inconclusive whether läkemedel if taken early in pregnancy results in reduced intelligence, neurodevelopmental problems, physical malformations in cardiac or facial structure, or other malformations in some newborns. läkemedel given to pregnant women antenatally may cause floppy infant syndrome^[74] in the neonate, or respiratory nedstämdhet necessitating ventilation.

  Regular läkemedel use during late pregnancy (the third trimester), carries a definite fara of benzodiazepine withdrawal syndrome in the neonate. Neonatal benzodiazepine withdrawal may include hypotonia, reluctance to suck, apneic spells, cyanosis, and impaired metabolic responses to cold stress. Symptoms of floppy infant syndrome and the neonatal benzodiazepine withdrawal syndrome have been reported to persist from hours to months after birth.^[75] läkemedel may also hämma fetal liver galla pigment glucuronidation, leading to neonatal jaundice.

  läkemedel fryst vatten present in breast milk, so caution must be exercised about breastfeeding.

Specific groups

[edit]

• Children and the elderly – The safety and effectiveness of läkemedel fryst vatten not well determined in children beneath 18 years of age, but it fryst vatten used to treat acute seizures.

  dos requirements have to be individualized, especially in people who are elderly and debilitated in whom the fara of oversedation fryst vatten greater. Long-term therapy may lead to cognitive deficits, especially in the elderly, which may only be partially reversible. The elderly metabolize benzodiazepines more slowly than younger people and are more sensitive to the adverse effects of benzodiazepines compared to younger individuals even at similar plasma levels.

  Additionally, the elderly tend to take more drugs which may interact or enhance the effects of benzodiazepines. Benzodiazepines, including läkemedel, have been funnen to increase the fara of falls and fractures in the elderly. As a result, dosage recommendations for the elderly are about half of those used in younger individuals and used for no längre than two weeks.^[22][76] läkemedel may also be slower to klar in the elderly, leading potentially to accumulation and enhanced effects.^[77] läkemedel, similar to other benzodiazepines and nonbenzodiazepines, causes impairments in body balance and standing steadiness in individuals who wake up at night or the next morning.

  Falls and hip fractures are frequently reported. The combination with alcohol increases these impairments. Partial, but incomplete, tolerance develops to these impairments.^[23]

• Liver or kidney failure – läkemedel may be safer than most benzodiazepines in people with impaired liver function. Like oxazepam, it does not require liver kemisk reaktion med syre, but only liver glucuronidation into lorazepam-glucuronide.

  Therefore, impaired liver function fryst vatten unlikely to result in läkemedel accumulation to an extent causing adverse reactions.^[40] Similarly kidney disease has minimal effects on läkemedel levels.^[78]

• Drug and alcohol dependence – The fara of abuse of läkemedel fryst vatten increased in dependent people.^[76]
• Comorbidpsychiatric disorders also increase the fara of dependence and paradoxical adverse effects.^[76]

Tolerance and dependence

[edit]

Dependence typified bygd a withdrawal syndrome occurs in about one-third of individuals who are treated for längre than fyra weeks with a benzodiazepine.

Higher doses and längre periods of use increase the fara of developing a benzodiazepine dependence. Potent benzodiazepines with a relatively short half-life, such as läkemedel, alprazolam, and triazolam, have the highest fara of causing dependence.^[22]

If regular treatment fryst vatten continued for längre than fyra to six months, dos increases may be necessary to maintain effects, but treatment-resistant symptoms may in fact be benzodiazepine withdrawal symptoms.^[79] Due to the development of tolerance to the anticonvulsant effects, benzodiazepines are generally not recommended for long-term use for the management of epilepsy.

Increasing the dos may overcome tolerance, but tolerance may then develop to the higher dos and adverse effects may persist and worsen. The mechanism of tolerance to benzodiazepines fryst vatten complex and involves GABA_A receptor downregulation, alterations to subunit configuration of GABA_A receptors, uncoupling, and internalization of the benzodiazepine binding site from the GABA_A receptor complex as well as changes in gene expression.^[22]

The likelihood of dependence fryst vatten relatively high with läkemedel compared to other benzodiazepines.

Lorazepam's relatively short serum half-life, its confinement mainly to blood, and its inactive metabolite can result in interdose withdrawal phenomena and next-dose cravings, that may reinforce psychological dependence. Because of its high potency, the smallest läkemedel platta strength of &#;mg fryst vatten also a significant dos.

To minimise the fara of physical/psychological dependence, läkemedel fryst vatten best used only short-term, at the smallest effective dos. If any benzodiazepine has been used long-term, the recommendation fryst vatten a gradual dos taper over a period of weeks, months or längre, according to dos and duration of use, the grad of dependence and the individual.

Coming off long-term läkemedel use may be more realistically achieved bygd a gradual switch to an equivalent dos of diazepam and a period of stabilization on this, and only then initiating dos reductions. The advantage of switching to diazepam fryst vatten that dos reductions are felt less acutely, because of the längre half-lives (20– hours) of diazepam and its active metabolites.^[80]

Withdrawal

[edit]

On abrupt or overly rapid discontinuation of läkemedel, anxiety, and signs of physical withdrawal have been observed, similar to those seen on withdrawal from alcohol and barbiturates.

läkemedel, as with other benzodiazepine drugs, can cause physical dependence, addiction, and benzodiazepine withdrawal syndrome.

How it works

The higher the dos and the längre the drug fryst vatten taken, the greater the fara of experiencing unpleasant withdrawal symptoms. Withdrawal symptoms can, however, occur from standard dosages and also after short-term use. Benzodiazepine treatment should be discontinued as soon as possible via a slow and gradual dos reduction regimen.^[81]Rebound effects often resemble the condition being treated, but typically at a more intense level and may be difficult to diagnose.

Withdrawal symptoms can range from mild anxiety and insomnia to more severe symptoms such as seizures and psychosis. The fara and severity of withdrawal are increased with long-term use, use of high doses, abrupt or over-rapid reduction, among other factors. Short-acting benzodiazepines such as läkemedel are more likely to cause a more severe withdrawal syndrome compared to longer-acting benzodiazepines.^[22]

Withdrawal symptoms can occur after taking therapeutic doses of läkemedel for as little as one week.^{[citation needed]} Withdrawal symptoms include headaches, anxiety, tension, nedstämdhet, insomnia, restlessness, confusion, irritability, sweating, dysphoria, dizziness, derealization, depersonalization, numbness/tingling of extremities, hypersensitivity to light, sound, and smell, perceptual distortions, nausea, vomiting, diarrhea, appetite loss, hallucinations, delirium, seizures, tremor, stomach cramps, myalgia, intensiv oro eller upprördhet, palpitations, tachycardia, panik attacks, short-term memory loss, and hyperthermia.

It takes about 18–36 hours for the benzodiazepine to be removed from the body.^[82] The ease of physical dependence to läkemedel, (Ativan brand was particularly cited), and its withdrawal were brought to the attention of the British public during the early s in Esther Rantzen's BBC TV series That's Life!, in a feature on the drug over a number of episodes.

Interactions

[edit]

Lorazepam fryst vatten not usually fatal in overdose, but may cause respiratory nedstämdhet if taken in overdose with alcohol. The combination also causes greater enhancement of the disinhibitory and amnesic effects of both drugs, with potentially embarrassing or criminal consequences. Some experts advise that people should be warned against drinking alcohol while on läkemedel treatment,^[44][83] but such klar warnings are not universal.^[84]

Greater adverse effects may also occur when läkemedel fryst vatten used with other drugs, such as opioids or other hypnotics.^[78] läkemedel may also interact with rifabutin.^[85]Valproate inhibits the metabolism of läkemedel, whereas carbamazepine, lamotrigine, phenobarbital, phenytoin, and rifampin increase its rate of metabolism.

Some antidepressants, antiepileptic drugs such as phenobarbital, phenytoin and carbamazepine, sedative antihistamines, opiates, antipsychotics and alcohol, when taken with läkemedel may result in enhanced sedative effects.^[22]

Overdose

[edit]

See also: Benzodiazepine overdose

In cases of a suspected läkemedel overdose, it fryst vatten important to establish whether the individ fryst vatten a regular user of läkemedel or other benzodiazepines since regular use causes tolerance to develop.

Also, one must ascertain whether other substances were also ingested.

Signs of overdose range through mental confusion, dysarthria, paradoxical reactions, drowsiness, hypotonia, ataxia, hypotension, hypnotic state, coma, cardiovascular nedstämdhet, respiratory nedstämdhet, and death. However, fatal overdoses on benzodiazepines alone are rare and less common than with barbiturates.^[86] Such a difference fryst vatten largely due to benzodiazepine activity as a neuroreceptor modulator, and not as an activator per titta.

läkemedel and similar medications do however act in synergy with alcohol, which increases the fara of overdose.

Early management of people beneath alert includes emetics, gastric lavage, and activated charcoal. Otherwise, management fryst vatten bygd insamling, including of grundläggande signs, support and, only if necessary, considering the hazards of doing so, giving intravenousflumazenil.

People are ideally nursed in a kind, frustration-free environment, since, when given or taken in high doses, benzodiazepines are more likely to cause paradoxical reactions. If shown sympathy, even ganska crudely feigned, people may respond solicitously, but they may respond with disproportionate aggression to frustrating cues.^[87] Opportunistic counseling has limited value here, as the individ fryst vatten unlikely to recall this later, owing to drug-induced anterograde amnesia.

Detection in body fluids

[edit]

Lorazepam may be quantitated in blood or plasma to confirm poisoning in hospitalized people, provide bevis of an impaired driving fängelse or to assist in a medicolegal death investigation. Blood or plasma concentrations are usually in a range of 10– μg/L in persons either receiving the drug therapeutically or in those arrested for impaired driving.

Approximately – μg/L fryst vatten funnen in people after acute overdosage.^[88] läkemedel may not be detected bygd commonly used urine drug screenings for benzodiazepines. This fryst vatten due to the fact that the majority of these screening tests are only able to detect benzodiazepines that undergo oxazepamglucuronide metabolism.^[89][90][91]

Pharmacology

[edit]

Lorazepam has anxiolytic, sedative, hypnotic, amnesic, anticonvulsant, and muscle relaxant properties.^[92] It fryst vatten a high-potency and an intermediate-acting^{[clarification needed]} benzodiazepine, and its uniqueness,^[93][94] advantages, and disadvantages are largely explained bygd its pharmacokinetic properties (poor vatten and lipid solubility, high protein binding and anoxidative metabolism to a pharmacologically inactive glucuronide form) and bygd its high relative potency (lorazepam 1&#;mg fryst vatten lika in effect to diazepam 10&#;mg).^[95][96] The biological half-life of läkemedel fryst vatten 10–20 hours.^[97]

Pharmacokinetics

[edit]

Lorazepam fryst vatten highly protein bound and fryst vatten extensively metabolized into pharmacologically inactive metabolites.^[22] Due to its poor lipid solubility, läkemedel fryst vatten absorberad relatively slowly bygd ingång and fryst vatten unsuitable for rectal ledning.

However, its poor lipid solubility and high grad of protein binding (85–90%^[98]) mean its volume of leverans fryst vatten mainly the vascular compartment, causing relatively prolonged peak effects. This contrasts with the highly lipid-soluble diazepam, which, although rapidly absorberad orally or rectally, soon redistributes from the serum to other parts of the body, in particular, body tallrik.

This explains why one läkemedel dos, despite its shorter serum half-life, has more prolonged peak effects than an equivalent diazepam dose.^[99] läkemedel fryst vatten rapidly conjugated at its 3-hydroxy group into läkemedel glucuronide which fryst vatten then excreted in the urine. läkemedel glucuronide has no demonstrable CNS activity in animals.

The plasma levels of läkemedel are proportional to the dos given. There fryst vatten no bevis of accumulation of läkemedel on ledning up to six months. On regular ledning, diazepam will accumulate, since it has a längre half-life and active metabolites, these metabolites also have long half-lives.

Lorazepam calms and sedates and may be used to treat anxiety, as an anticonvulsant, or for its sedative effects

Clinical example: Diazepam has long been a drug of choice for ställning eller tillstånd epilepticus; its high lipid solubility means it gets absorberad with lika speed whether given orally, or rectally (nonintravenous routes are convenient outside of hospital settings), but diazepam's high lipid solubility also means it does not remain in the vascular space, but soon redistributes into other body tissues.

So, it may be necessary to repeat diazepam doses to maintain peak anticonvulsant effects, resulting in excess body accumulation. läkemedel fryst vatten a different case; its low lipid solubility makes it relatively slowly absorberad bygd any rutt other than intravenously, but once injected, it will not get significantly redistributed beyond the vascular space. Therefore, lorazepam's anticonvulsant effects are more durable, thus reducing the need for repeated doses.

If a individ fryst vatten known to usually stop convulsing after only one or two diazepam doses, it may be preferable because sedative after effects will be less than if a single dos of läkemedel fryst vatten given (diazepam anticonvulsant/sedative effects wear off after 15–30 minutes, but läkemedel effects gods 12–24 hours).^[] The prolonged sedation from läkemedel may, however, be an acceptable trade-off for its reliable duration of effects, particularly if the individ needs to be transferred to another facility.

Although läkemedel fryst vatten not necessarily better than diazepam at initially terminating seizures,^[] läkemedel fryst vatten, nevertheless, replacing diazepam as the intravenous agent of choice in ställning eller tillstånd epilepticus.^[][]

Lorazepam serum levels are proportional to the dos administered. Giving 2&#;mg oral läkemedel will result in a peak total serum level of around 20&#;ng/mL around two hours later,^[98][] half of which fryst vatten läkemedel, half its inactive metabolite, lorazepam-glucuronide.^[] A similar läkemedel dos given intravenously will result in an earlier and higher peak serum level, with a higher relative proportion of unmetabolised (active) lorazepam.^[] On regular ledning, maximum serum levels are attained after three days.

Longer-term use, up to six months, does not result in further accumulation.^[98] On discontinuation, läkemedel serum levels become negligible after three days and undetectable after about a week.

Medically reviewed by Carmen Pope, BPharm

läkemedel fryst vatten metabolized in the liver bygd conjugation into inactive lorazepam-glucuronide. This metabolism does not involve liver kemisk reaktion med syre, so fryst vatten relatively unaffected bygd reduced liver function. Lorazepam-glucuronide fryst vatten more water-soluble than its precursor, so gets more widely distributed in the body, leading to a längre half-life than läkemedel.

Lorazepam-glucuronide fryst vatten eventually excreted bygd the kidneys,^[98] and, because of its tissue accumulation, it remains detectable, particularly in the urine, for substantially längre than läkemedel.

Pharmacodynamics

[edit]

Relative to other benzodiazepines, läkemedel fryst vatten thought to have high affinity for GABA receptors,^[] which may also explain its marked amnesic effects.^[44] Its main pharmacological effects are the enhancement of the effects of the neurotransmitter GABA at the GABA_A receptor.^[22] Benzodiazepines, such as läkemedel, enhance the effects of GABA at the GABA_A receptor via increasing the frequency of opening of the chloride ion kanal on the GABA_A receptors; which results in the therapeutic actions of benzodiazepines.

They, however, do not on their own activate the GABA_A receptors, but require the neurotransmitter GABA to be present. Thus, the effect of benzodiazepines fryst vatten to enhance the effects of the neurotransmitter GABA.^[22][78]

The magnitude and duration of läkemedel effects are dose-related, meaning larger doses have stronger and longer-lasting effects, because the brain has spare benzodiazepine drug receptor capacity, with single, clinical doses leading only to an occupancy of some 3% of the available receptors.^[]

The anticonvulsant properties of läkemedel and other benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.

Sustained repetitive firing seems to get limited, bygd the benzodiazepine effect of slowing recovery of sodium channels from inactivation to deactivation in mouse spinal cord fängelse cultures, hence prolonging the refractory period.^[]

Physical properties and formulations

[edit]

Pure läkemedel fryst vatten an almost vit powder that fryst vatten nearly insoluble in vatten and oil.

In medicinal struktur, it fryst vatten mainly available as tablets and a solution for injection, but, in some locations, it fryst vatten also available as a skin patch, an oral solution, and a sublingual platta.

Lorazepam tablets and syrups are administered orally. läkemedel tablets of the Ativan brand also contain lactose, microcrystalline cellulose, polacrilin, magnesium stearate, and coloring agents (indigo carmine in blue tablets and tartrazine in yellow tablets).

läkemedel for injection formulated with polyethylene glycol in propylene glycol with % benzyl alcohol as preservative.

Lorazepam injectable solution fryst vatten administered either bygd deep intramuscular injection or bygd intravenous injection. The injectable solution comes in 1 mL ampoules containing 2 or 4&#;mg of läkemedel.

The solvents used are polyethylene glycol and propylene glycol. As a preservative, the injectable solution contains benzyl alcohol.^[] Toxicity from propylene glycol has been reported in the case of a individ receiving a continuous läkemedel infusion.^[] Intravenous injections should be given slowly and they should be closely monitored for side effects, such as respiratory nedstämdhet, hypotension, or loss of airway control.

Peak effects roughly coincide with peak serum levels,^[] which occur 10 minutes after intravenous injection, up to 60 minutes after intramuscular injection, and 90 to minutes after oral administration,^[98][] but första effects will be noted before this.

Lorazepam är ett läkemedel som ofta används vid behandling av vissa kliniska tillstånd

A clinically betydelsefull läkemedel dos will normally be effective for six to 12 hours, making it unsuitable for regular once-daily ledning, so it fryst vatten usually prescribed as two to fyra daglig doses when taken regularly, but this may be extended to fem or six, especially in the case of elderly people who could not handle large doses at once.

Topical formulations of läkemedel, while sometimes used as treatment for nausea especially in people in ett hem eller vårdinrättning för terminalt sjuka patienter, has been advised against bygd the American Academy of ett hem eller vårdinrättning för terminalt sjuka patienter and Palliative medicin for this purpose as it has not been proven effective.^[]

History

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Historically, läkemedel fryst vatten one of the "classical" benzodiazepines.

Others include diazepam, clonazepam, oxazepam, nitrazepam, flurazepam, bromazepam, and clorazepate.^[] läkemedel was first introduced bygd Wyeth Pharmaceuticals in beneath the brand names Ativan and Temesta.^[] The drug was developed bygd D.J. Richards, president of research. Wyeth's original patent on läkemedel fryst vatten expired in the United States.

Society and culture

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Recreational use

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See also: Benzodiazepine misuse

Lorazepam fryst vatten also used for other purposes, such as recreational drug use, wherein it fryst vatten taken to achieve a high, or when the medicinering fryst vatten continued long-term against medical advice.^[]

A large-scale, nationwide, US government study of pharmaceutical-related emergency department visits bygd SAMHSA funnen sedative-hypnotics are the pharmaceuticals most frequently used outside of their prescribed medical purpose in the United States, with 35% of drug-related emergency department visits involving sedative-hypnotics.

In this category, benzodiazepines are most commonly used. Males and females use benzodiazepines for nonmedical purposes equally. Of drugs used in attempted suicide, benzodiazepines are the most commonly used pharmaceutical drugs, with 26% of attempted suicides involving them. läkemedel was the third-most-common benzodiazepine used outside of prescription in these ER visit statistics.^[]

Legal status

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Lorazepam fryst vatten a Schedule IV drug beneath the Controlled Substances Act in the US and internationally beneath the United Nations Convention on Psychotropic Substances.^[] It fryst vatten a Schedule IV drug beneath the Controlled Drugs and Substances Act in Canada.

In the United Kingdom, it fryst vatten a Class C, Schedule 4 Controlled Drug beneath the Misuse of Drugs Regulations ^[]

Pricing

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In , the US drug company Mylan agreed to pay US$ million to settle accusations bygd the Federal Trade kommission (FTC) that they had raised the price of generic läkemedel bygd % and generic clorazepate bygd % in after having obtained exclusive licensing agreements for certain ingredients.^[]

References

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