Protease inhibitors Health Dictionary

Protease Inhibitors: From 1 Different Sources


A new group of drugs which, in combination with antiviral agents, are used to treat AIDS (see AIDS/HIV). They inhibit the activity of PROTEASE, an enzyme produced by HIV, and which breaks down proteins. The drugs have recently been introduced: those in use are indinavir, nel?navir, ritonavir and saquinavir.
Health Source: Medical Dictionary
Author: Health Dictionary

Protease

A digestive ENZYME – also known as a proteolytic enzyme – that breaks down PROTEIN in food as part of the digestive process. The complex protein molecules are reduced to their constituent AMINO ACIDS.... protease

Proton-pump Inhibitors

These are drugs that inhibit the production of acid in the stomach by blocking a key enzyme system, known as the PROTON PUMP, of the parietal cells of the stomach. The drugs include omeprazole, lansoprazole and pantoprazole, and they are the treatment of choice for oesophagitis (erosion and stricture – see under OESOPHAGUS, DISEASES OF); for the short-term treatment for gastric ulcer (see under STOMACH, DISEASES OF) and DUODENAL ULCER; and, in combination with ANTIBIOTICS, for the eradication of Helicobacter pylori.... proton-pump inhibitors

Ace Inhibitors

See ANGIOTENSIN-CONVERTING ENZYME (ACE) INHIBITORS.... ace inhibitors

Angiotensin-convertingenzyme (ace) Inhibitors

The ENZYME that converts angiotensin I to angiotensin II (see ANGIOTENSIN) is called angiotensin-converting enzyme. Angiotensin II controls the blood pressure and is the most potent endogenous pressor substance produced in the body; angiotensin I has no such pressor activity. Inhibition of the enzyme that converts angiotensin I to angiotensin II will thus have marked effects on lowering the blood pressure, and ACE inhibitors have a valuable role in treating heart failure when thiazides and beta blockers cannot be used or fail to work, especially after myocardial infarction (see HEART, DISEASES OF). Captopril was the ?rst ACE inhibitor to be synthesised: it reduces peripheral resistance by causing arteriolar dilatation and thus lowers blood pressure. Other drugs such as enalapril, lisinopril, cilazapril, quinapril and ramipril have since been developed. Some kidney disorders increase the production of angiotensin II and so cause HYPERTENSION.... angiotensin-convertingenzyme (ace) inhibitors

Aromatase Inhibitors

A group of drugs that stop the action of the ENZYME, aromatase. This enzyme converts androgens (see ANDROGEN) to OESTROGENS. If this conversion is inhibited, the concentrations of oestrogens in the body are reduced – so these drugs operate against tumours, such as breast cancer, that depend on oestrogen for their growth. Aromatase inhibitors include anastrazole and formestane, and they are usually prescribed as second-line treatment after TAMOXIFEN, the prime drug treatment for breast cancer.... aromatase inhibitors

Cox-2 Inhibitors

This stands for cyclo-oxygenase 2 inhibitors – a class of drugs used in treating ARTHRITIS – of which the most well-used is celecoxib. Their main claim is that they are less likely to cause gastrointestinal disturbance than NONSTEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDS). In 2001, the National Institute for Clinical Excellence (NICE) recommended that they should not be used routinely in rheumatoid arthritis or osteoarthritis but only in patients with a history of peptic ulcer or gastrointestinal bleeding. They should also be considered in persons over the age of 65 taking other drugs which could cause gastrointestinal bleeding, those who are very debilitated, and those who are taking maximum doses of NSAIDs. In 2005, rofecoxib was withdrawn because of concerns about cardiac side-effects.... cox-2 inhibitors

Cyclo-oxygenase-2 Selective Inhibitors

See COX-2 INHIBITORS.... cyclo-oxygenase-2 selective inhibitors

Monoamine Oxidase Inhibitors (maois)

These are drugs that destroy, or prevent the action of, monoamine oxidase (MAO). Monoamines, which include NORADRENALINE and tyramine, play an important part in the metabolism of the BRAIN, and there is some evidence that excitement is due to an accumulation of monoamines in the brain. MAO is a naturally occurring ENZYME which is concerned in the breakdown of monoamines. MAOIs were among the earliest ANTIDEPRESSANT DRUGS used, but they are now used much less than tricyclic and related antidepressants, or SELECTIVE SEROTONIN-REUPTAKE INHIBITORS (SSRIS) and related antidepressants, because of the dangers of dietary or drug interactions – and because MAOIs are less e?ective than these two groups.

An excessive accumulation of monoamines can induce a dangerous reaction characterised by high blood pressure, palpitations, sweating and a feeling of su?ocation. Hence the care with which MAOI drugs are administered. What is equally important, however, is that in no circumstances should a patient receiving any MAOI drug eat cheese, yeast preparations such as Marmite, tinned ?sh, or high game. The reason for this ban is that all these foodstu?s contain large amounts of tyramine which increases the amount of certain monoamines such as noradrenaline in the body. (See MENTAL ILLNESS.)

There are also certain drugs, such as AMPHETAMINES and PETHIDINE HYDROCHLORIDE, which must not be taken by a patient who is receiving an MAOI drug. The MAOIs of choice are phenelzine or isocarboxazid because their stimulant effects are less than those of other MAOIs, making them safer.... monoamine oxidase inhibitors (maois)

Selective Serotonin-reuptake Inhibitors (ssris)

These ANTIDEPRESSANT DRUGS have few antimuscarinic effects (see ANTIMUSCARINE), but do have adverse effects of their own – predominantly gastrointestinal. They are, however, much safer in overdose than the tricyclic antidepressants, which is a major advantage in patients who are potentially suicidal. Examples are citalopram, used to treat panic disorders, as well as depressive illness; FLUOXETINE; and PAROXETINE. (See also MENTAL ILLNESS.)... selective serotonin-reuptake inhibitors (ssris)

Dopa-decarboxylase Inhibitors

Drugs used in the treatment of Parkinson’s disease.

The 2 main dopa-decarboxylase inhibitors, co-beneldopa and co-careldopa, are a combination of levodopa and benserazide and levodopa and carbidopa respectively.

These drugs prevent levodopa from being activated except within the brain, which reduces the incidence of side effects such as nausea and vomiting.... dopa-decarboxylase inhibitors

Monoamine Oxidase Inhibitors

Also known as MAOIs, one of the 3 main types of antidepressant drug.

They work by preventing the breakdown of certain neurotransmitters by the enzyme monoamine oxidase.

The increased levels of neurotransmitters that result are associated with improved mood.

Common drugs include phenelzine and isocarboxazid.

All MAOIs interact with certain other drugs and foods such as cheese and red wine; but moclobemide is known as a reversible , which makes the adverse reactions less likely to occur.... monoamine oxidase inhibitors

Acetylcholinesterase Inhibitors

A group of drugs that are used in the treatment of mild to moderate dementia due to Alzheimer’s disease, in which there is a deficiency of the neurotransmitter acetylcholine in the brain.

Drugs such as donepezil and rivastigmine work by blocking the action of acetylcholinesterase, the enzyme in the brain responsible for the breakdown of acetylcholine.

This raises acetylcholine levels, and, in half of all patients, the drugs slow the rate of progression of dementia.

They have no effect on dementia due to other causes, such as stroke or head injury, however.

Common side effects include nausea, dizziness, and headache.

Rarely, difficulty in passing urine may occur.... acetylcholinesterase inhibitors

Reverse Transcriptase Inhibitors

A class of drugs used in the treatment of diseases, including HIV infection, that are caused by retroviruses. The drugs affect the ability of the virus to reproduce by blocking reverse transcriptase, a key enzyme. Drugs include lamivudine, zidovudine (AZT), efavirenz, and stavudine.... reverse transcriptase inhibitors

Selective Serotonin Reuptake Inhibitors

(SSRIs) A relatively new class of drugs that are used to treat depression.

They work by blocking the reabsorption of the neurotransmitter serotonin following its release in the brain.

The increased serotonin levels that result are associated with improved mood.

Common drugs in this group include fluoxetine and sertraline.

SSRIs are usually taken orally once a day; it may take 1–3 weeks for any noticeable improvement in symptoms.

SSRIs usually produce fewer side effects than other types of antidepressant drug.

However, they may cause diarrhoea, nausea, restlessness, and anxiety.... selective serotonin reuptake inhibitors

Calcineurin Inhibitors

drugs that act by inhibiting the calcium-dependent protein *phosphatase calcineurin, an enzyme that initiates a sequence of events that bring about activation of T *lymphocytes. The group includes *ciclosporin and *tacrolimus, which are major maintenance immunosuppressants used in transplantation. Topical calcineurin inhibitors (e.g. tacrolimus, pimecrolimus [Elidel]) are used in the treatment of eczema when topical steroids have failed or are contraindicated. Stinging is a common transient side-effect, and reactivation of infections may occur.... calcineurin inhibitors

Dpp-iv Inhibitors

a group of *oral hypoglycaemic drugs used in the treatment of type 2 diabetes mellitus. Through inhibiting the enzyme dipeptidyl peptidase-IV they enhance the action of *glucagon-like peptide-1. Five drugs in this group are currently licensed for use in the UK: sitagliptin, vildagliptin, saxagliptin, linagliptin, and alogliptin.... dpp-iv inhibitors

Protease Inhibitor

any one of a class of drugs used in the treatment of HIV infection and *AIDS. Used in combination with other *antiretroviral drugs, they act by inhibiting the action of protease, an enzyme produced by HIV that cleaves two precursor proteins into smaller fragments. These fragments are required for viral growth, infectivity, and replication. Protease inhibitors include atazanavir, indinavir, lopinavir and ritonavir (which are used in combination), saquinavir, and tipranavir. Side-effects include nausea, vomiting, diarrhoea, and rashes; these drugs are also associated with hyperglycaemia and *lipodystrophy. See also boceprevir.... protease inhibitor

Sglt-2 Inhibitors

a class of *oral hypoglycaemic drugs for use in the treatment of type 2 diabetes mellitus. Sodium/glucose cotransporter 2 (SGLT-2) plays the largest role in glucose reabsorption in the kidney. Inhibition of SGLT-2 leads to an increase in the loss of glucose in the urine, a reduction in blood glucose levels, and a modest degree of weight loss over time due to the increased calorie loss. Two drugs in this class are currently licensed for use in the UK: dapagliflozin (Forxiga) and canagliflozin (Invokana).

SGOT (serum glutamic oxaloacetic transaminase) see aspartate aminotransferase.

SGPT (serum glutamic pyruvic transaminase) see alanine aminotransferase.... sglt-2 inhibitors

Topical Calcineurin Inhibitors

see calcineurin inhibitors.... topical calcineurin inhibitors



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