Fibrates mechanism of action indications and use of drugs

So what is fibrate? This is a group of pharmaceuticals that helps lower plasma fat levels, as well as normalize lipid metabolism with it. For the first time, this medicine based on fibroic acid was used in the treatment of people in 1962. If we talk about today’s diversity of this group, then their number corresponds to ten.

Very often, doctors prescribe statins as a concomitant drug. Both of them have a beneficial effect on the normalization of the fat content in the patient’s body. It is important that only a doctor can prescribe the medicine correctly!

Fibrates are prescribed to normalize fat metabolism in the body.

Influence on the body

During the course of treatment, blood circulation and metabolism are restored. If diseases of the cardiovascular system occur against the background of diabetes mellitus, then their administration avoids various complications. Also, drugs are indicated for people with gangrene and retinopathy.

Xanthine derivatives: teufillin, aminophylline (aminophylline).

Pharmacodynamics: Being
phosphodiesterase and purine inhibitors
receptors, increase cAMP levels.
reduce the concentration of Ca ions and cause
vasodilating effect of blood circulation
in internal organs (including
kidneys) is improving. Thanks to this
action, filtration ability
glomeruli increases, urine flow through the nephron
accelerates, the contact time of Na ions with
renal tubule epithelium is reduced
and, as a consequence of this, decreases
elimination reabsorption
from the body of water, sodium ions and chlorine.

Application
Cardiovascular congestion
insufficiency.

Complications. Head
pain, dizziness, central nervous system agitation,
convulsions, tachycardia, bradycardia (with
intravenous administration), nausea ,. vomiting
pain in the epigastric region.

The mechanism of action of fibrates

Antihypertensive
(antihypertensive) agents are substances
different structure, therefore more often
classified by mechanism of action,
not by chemical structure.

Antihypertensive
funds lower blood pressure
various mechanisms. Pressure in
any piping system with which
conditionally it is possible to compare CCC, depends on
the volume of fluid in it, the width of the lumen
pipes (vessels) and pump power
(hearts). Antihypertensive drugs reduce
circulating blood volume, increase
vascular lumen width and thereby
reduce total peripheral resistance
(OPS). They also reduce the strength of the heart.
contractions and cardiac output.

The mechanism of action of fibrates is based on the high activity of the enzyme (lipoprotein lipase), which breaks down LDL and VLDL, while the hepatic metabolism is restored and increased fat metabolism. All this is aimed at reducing the risk of emergence and complications of vascular atherosclerosis, which leads to disability and early death due to the accumulation of cholesterol in all major, large vessels. And the most dangerous complications of this disease (cerebral stroke and heart attack) can be fatal.

Fibrates (derivatives of fibroic acid) have a multiple effect on lipid formation processes. They reduce the synthesis of triglycerides included in VLDL and increase the activity of the LPL enzyme, which breaks down VLDL. These two effects lead to a decrease in blood levels of VLDL and triglycerides.

Fibrate therapy is accompanied by a clear increase in HDL. It was noted that fibrates have a wide range of favorable non-lipid (pleiotropic) effects, among which anti-inflammatory, antioxidant, anticoagulant properties, and the effect on vascular tone endothelial regulation are of particular interest.

Osmotic diuretic: attracts.

Pharmacodynamics: Diuretic
effect due to limitation
reabsorption of water in the proximal
tubules and increased osmotic
plasma pressure. Due to counteracting
osmotic force volume increases
have urine with excretion. Relevant
an increase in urine flow rate reduces
the time of her contact with the tubular epithelium,
which reduces subsequent reabsorption
Na ions.

Application: Docking
cerebral and pulmonary edema. Expression
dehydrating effect is manifested
only with filtration ability
the kidneys.

Glaucoma.
Decreased intracranial and intraocular
pressure is associated not only with diuretic
effect, but also with a central effect
(activation of osmoreceptive fields
hypothalamus under the action of hypertonic
solution). Relieving seizures, effect
due to strong dyshydrogenation
action and decreased intracranial
pressure.

Complications. Head
pain, dizziness, dyspepsia,
dehydration (thirst, cyxos in the mouth),
hypernatremia, osmotic diarrhea.
Heart failure and
pulmonary edema due to the fact. what u
patients with severe disease
kidneys, urine may not form
even with osmotic load, and in this
hypertonic solution causes
increase in circulating blood volume.

Loopback
diuretics: furosemide (lasix), ethacrine
acid (yregite), bumetanide (bufenoks),
torsemide (used abroad).

Formacodynamics. Suppress
combined transport system Na, K,
Cl- in the apical (facing the lumen
tubule) membrane thick ascending
parts of the Henry loop, i.e. reduce reabsorption
Na, Cl-. Increased prostacyclin levels
(Pg. I2) in the coronary and peripheral
vessels helps reduce pressure.

Application. Edema
lung and brain cirrhosis. Using
associated with the ability to reduce volume
(Bcc) and reduce stagnation in
small and large circle of blood circulation.
Hypertension
BCC, allows to reduce peripheral
vascular resistance (OPSS) and
lower blood pressure.

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Antihypertensive effect is enhanced
due to the accumulation in the vessels of endogenous
PG! 2, with vasodilator
properties. Anion poisoning
Efficacy for bromide poisoning,
fluorides, iodides, due
the ability of the latter to reabsorb
in the thick section of the ascending part of the loop
Henle (in the scope of loop
diuretics).

Complications Hypokalemic
metabolic alkalosis, hyperuricemia
and the provocation of gout attacks,
hypomagnesemia, hypocalcemia,
ototoxic effect (especially in
combined with antibiotics from the group
aminoglycaseides), allergic
reaction.

Противопоказания

Preparations from the fibrate group are indicated for individuals with type II, type III, type IV, type V hyperlipidemia, as well as those who have low HDL cholesterol in combination with high LDL cholesterol and high triglycerides. Fibrates reduce triglyceride levels by 30-50%, LDL by 10-15% and increase the concentration of HDL by 10-20%

Preparations
iron – a group of medicinal
products containing salts or complexes
bivalent and trivalent iron, and
their combinations with other drugs. IN
mainly used to treat and
prophylaxis of iron deficiency anemia.
Vanatomotherapeutic
classifications merged under code
B03A.

Combined
drugs in this group
must contain at least 30 mg of the main
active substance in terms of
elemental iron, otherwise
they cannot be used in treatment
iron deficiency states and will
classified as vitamins or
general tonic agents.

In general,
this category of drugs
can be divided into several main
groups: salt-based preparations
ferrous and ferric iron,
various iron complexes
and combination agents. Preparations
of iron salts are prescribed only
orally.

Sorbifer
durules, tardiferon (folate sulfate
acid). Two tablets are used
per day (morning and evening), half an hour before
food, drink a glass of water.

Actiferrin
Hemofer, Ferronal, Totem. Accept
30 minutes before meals, between meals, s
vitamin fruit juice
C, to improve the absorption of iron.

Fenyuls
available in capsules, taken 1 time
in a day. With heavy menstruation
taken 2 days before and after menstruation
1 capsule per day

Heferol
Ferrogradumet, Ferroplex, etc.

Ferrum
Lek taken with food, you can
mix with fruit juices and mashed potatoes.
You can divide the daily dose into
several tricks can be taken in one
reception.

Ferlatum
– this is a solution, it is taken before meals
1 bottle per day in two divided doses.

Fefol
1 capsule 1 hour before a meal.

Maltofer
– the dose is calculated individually
according to the table, before use they recommend
test for adverse reactions
organism.

Preparations
iron are shown at [1]:

iron deficiency
conditions (main indication);

with
intolerance to cow’s milk;

children
acute or prolonged
infectious diseases.

Deficit
iron can be caused [1]:

insufficient
the intake of iron in the fetus
(with feto-fetal and feto-maternal
transfusion), child or adult
human;

violation of
intestinal absorption
(malabsorption syndrome, inflammatory
processes in the intestine, against the background of taking
tetracycline antibiotics and
other drugs);

sharp
massive or chronic
blood loss (bleeding, helminths
infestations, nasal hemorrhages, juvenile
uterine bleeding, prolonged
hematuria and others);

result
increased iron consumption (period
infectious growth
diseases and others).

Fibrates are hypolipidemic agents, and they are indicated for the use of the following categories of people:

  • people with high cholesterol;
  • at risk due to hereditary indicators;
  • patients for whom diet did not help lower cholesterol.

Fibrates are contraindicated in people with gallstone disease, liver or kidney failure, and others. Pregnant women and children under 18 years of age should also not take these drugs. Older people and alcohol abusers should take them on a limited basis.

They can not be used with nephro and hepatotoxic drugs, anticoagulants. Properly selected dosage contribute to the easy perception of patients. Side effects from fibrates are diagnosed in 10% of people.

Summing up, it is worth noting that modern technology has significantly reduced the side effects that occur during treatment. This class of drugs is a good tool for normalizing cholesterol, is a prophylactic for atherosclerosis, and also has a tonic effect.

The independent use of fibrates can bring the main systems and organs to a pathologically dangerous state. The correct combination of it with a diet (low in fat) and moderate physical activity for a long time will prolong life and health.

The list of types of fibrates is large, so we will get acquainted with its main representatives:

  • Clofibrate – this medicine was previously used as a prophylactic against coronary sclerosis, angiopathy (diabetic). This is the very first form of this orientation was first used for treatment in the sixties. Currently, it is not used, since the list of side effects is very large. The most dangerous of them is myositis.
  • The next representative – Gemfibrozil, also has a number of side effects. This capsule or tablet preparation is available in two forms of 450 and 650 mg.
  • Fenofibrate is recognized as a universal remedy for lowering cholesterol. In addition to non-lipid actions, it has an anti-inflammatory effect, an antioxidant and tonic.
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Fenofibrate

A huge number of well-known pharmaceutical companies produce various chemical combinations of this group. In post-Soviet countries, fibrates are replaced with statins.

How to use

Instructions for the use of fibrates: the course of treatment with these medications is long. Depending on the patient’s individual indicators, doctors prescribe 2-3 tablets or capsules per day. Their intake is necessarily combined with a special diet and periodic clinical and laboratory studies. To enhance the effect, tablets are taken before meals or during.

Fibrate Dosage Table

When using them, discomfort may occur in the gastrointestinal tract, headache, rash, dermatitis, dry mouth, dyspepsia, anemia may occur. There are problems with potency and decreased libido. With an independent (without consulting a doctor) appointment, complications and disturbances in the work of the most important organs and systems (central nervous system, heart, liver, bone skeleton, muscles) are likely.

The main drugs of fibrates, their benefits and harms

Detonic – a unique medicine that helps fight hypertension at all stages of its development.
Detonic for pressure normalization

The complex effect of plant components of the drug Detonic on the walls of blood vessels and the autonomic nervous system contribute to a rapid decrease in blood pressure. In addition, this drug prevents the development of atherosclerosis, thanks to the unique components that are involved in the synthesis of lecithin, an amino acid that regulates cholesterol metabolism and prevents the formation of atherosclerotic plaques.

Detonic not addictive and withdrawal syndrome, since all components of the product are natural.
Detailed information about Detonic is located on the manufacturer’s page www.detonicnd.com.

Gemfibrozil

Of this group, gemfibrozil is best studied. Its use leads to a significant reduction in triglycerides and, to a lesser extent, cholesterol. A distinctive feature of gemfibrozil is the ability to increase HDL cholesterol in the blood. Long-term use of the drug (two years or more) due to its main effects ensures a decrease in blood lipids and, as a consequence, a decrease in the likelihood of developing myocardial infarction and death from it in type II hyperlipidemia.

Side effects of gemfibrozil:

  • желудочно-кишечные расстройства
  • dyspepsia
  • stomach ache
  • leukopenia
  • thrombocytopenia
  • anemia
  • Lipanor (ciprofibrate) has an effective long-term effect, starting from the twelfth week of treatment, reducing total cholesterol by 29%, triglycerides – by 42%. Treatment with lipanor allows you to restore the normal lipoprotein profile of blood plasma by reducing the content of VLDL and LDL with a simultaneous increase in the number of HDL.

    The decrease in cholesterol and triglycerides under the action of lipanor is accompanied by a significant decrease in the level of fibrinogen and an increase in physiological fibrinolytic activity. Unlike preparations of the fibrate group, long-term use of lipanor is well tolerated, there is no significant increase in the risk of stone formation in the gallbladder.

    Side effects of using lipanor:

  • moderate increase in transaminase levels
  • alkaline phosphatase reduction
  • Fibroic Acid Derivatives (Fibrates)
    Name Доза Note
    Bezafibrat
    (no-alip, no-amidine)
    200 mg x
    2-3 times / day
    400 mg per day
    (slow release form)
    Gemfibrozil 600 mg x
    2 times / day
    Maybe 900-1500 mg / day
    Ciprofibrate
    (lipanor)
    100 mg x 1-2 times / day 200 mg / day possible
    Fenofibrate
    (lipantyl)
    200 mg x
    1 time / day
    In the form of a micronized form 200 mg 1 time / day

    Blockers
    angiotensin II receptors – one of
    new classes of drugs to normalize
    blood pressure. Names
    preparations of this group end
    to “-artan.” Their first representatives
    synthesized in the early 90s of the twentieth
    centuries. Receptor blockers
    angiotensin II inhibit activity
    renin-angiotensin-aldosterone
    systems, thereby contributing to the whole
    a number of positive effects.

    The main
    indications for using blockers
    angiotensin II receptors serve as AH and
    chronic heart failure.
    They are significantly inferior in their activity
    ACE inhibitors.

    “Losartan.”
    Eprosartan. Irbesartan
    Telmisartan. “Valsartan.”
    Candesartan

    Показания
    to the application

    Accept
    substances of this group can only be
    the appointment of the attending physician. Exist
    a few cases in which it would be
    reasonable use of receptor blockers
    angiotensin 2.

    Hypertension. This disease is considered
    The main indication for the use of sartans.
    This is due to the fact that blockers
    angiotensin 2 receptors do not exert
    negative effects on metabolism,
    do not provoke erectile dysfunction,
    do not worsen bronchial patency.
    The action of the drug begins already
    two to four weeks after
    start treatment.

    Heart
    deficiency receptor blockers
    angiotensin 2 inhibit action
    renin-angiotensin-aldosterone
    systems whose activity provokes
    development of the disease. Nephropathy. Due to diabetes and
    arterial hypertension occur
    serious malfunctions
    the kidneys. Angiotensin Receptor Blockers
    2 protect these internal organs and do not
    allow you to output too much protein
    with urine.

    Tatyana Jakowenko

    Editor-in-chief of the Detonic online magazine, cardiologist Yakovenko-Plahotnaya Tatyana. Author of more than 950 scientific articles, including in foreign medical journals. He has been working as a cardiologist in a clinical hospital for over 12 years. He owns modern methods of diagnosis and treatment of cardiovascular diseases and implements them in his professional activities. For example, it uses methods of resuscitation of the heart, decoding of ECG, functional tests, cyclic ergometry and knows echocardiography very well.

    For 10 years, she has been an active participant in numerous medical symposia and workshops for doctors - families, therapists and cardiologists. He has many publications on a healthy lifestyle, diagnosis and treatment of heart and vascular diseases.

    He regularly monitors new publications of European and American cardiology journals, writes scientific articles, prepares reports at scientific conferences and participates in European cardiology congresses.

    Detonic