Peculiarities of pharmacotherapy of older

1,2 billion people. In this
expected to increase the number of those who will be in 80 years, farmorethan
now, and will become a 100-year-olds. According to recent studies,
number of old people (75 - 80 years) on our planet is increasing annually at
2,4%.
Age and Russians. So, people of retirement age in our country in 1998
there were about 30 million people, representing an average of 20% (and in many regions
already approaching 30%) of the total population, and over the years
number of such people will increase. This will require further development not only
gerontology and geriatric services, including geriatric pharmacology
. And here's why.
Believed that on average one patient aged 60 found
four or five different diseases that naturally accompanied by increased consumption of such a patient
variety of medicines. However, in the body
older people often change pharmacodynamics and pharmacokinetics
dasgs have significantly higher incidence of side effects.
Ignorance is a doctor that can aggravate the disease in elderly patients.
therefore now very urgent task is to master the medical
various ad hoc geriatric pharmacology.
Each physician should have a clear understanding of the principles
dispensing of dasgs in geriatrics and peculiarities of the interaction of dasgs on
ways to enhance the body's resistance of older persons to undesirable effects of dasgs
.
Before appoint medicine
question of appointment of any dasg should only be tackled
after a comprehensive analysis of its impact on the body an elderly patient. When
this must first take into account the increased sensitivity of elderly and old people
to dasgs (particularly to cardiac glycosides, hypotensive
Dasgs, tranquilizers, antidepressants), as well as a mental state
sick and conditions which he lives.
Another important asle of geriatric pharmacotherapy is strict
individualization of doses. At the beginning of the treatment dasg is prescribed in doses,
reduced approximately 2-fold compared with those for patients
middle age. And only gradually increasing the dose, set individual
tolerability. Upon reaching the therapeutic effect, reduce the dose to
supportive, which is usually also lower the dose prescribed to patients
middle age.
Must be remembered that the way the medication should be as easy as possible for
patient. If possible, avoid use of liquid dosage forms,
because of the weakened vision and shaky hands elderly patients experiencing difficulties with their
dosage. In addition, the lack of a clear monitoring
integrity bottle can lead to changes in the concentration of the dasg, its
contamination or deterioration.
In a hospital medical staff should pay particular attention to monitoring
timely reception of prescribed medications, since older and old people
often forget to take medicine on time or, conversely, take it
again, without waiting for the appointed time.
Pharmacological metamorphosis

In the body of elderly patients significantly altered pharmacokinetics and pharmacodynamics
dasgs. It was found that the older
organism, the greater the likelihood of intoxication even when appointing
dasgs in high therapeutic doses. In these patients, slowing
absorption from the gastrointestinal tract, the distribution of medicines
means in the body, violated their binding to blood proteins, reduced the rate of biotransformation
dasgs in the liver, slows the removal of parts of
organism.
Emerging aging stasctural and functional changes
gastrointestinal tract predispose to lower and slower income
dasgs in the blood. As a result of slower onset of effect when taking such,
example, dasgs such as barbiturates, tranquilizers, tricyclic antidepressants
, antiparkinsonian means, tetracycline antibiotics.
But constipation leads, conversely, to enhance absorption of dasgs.
Receiving atropine platifillina, fenotiazinovyh neuroleptics possessing
M-anticholinergic effects, other dasgs that cause slowing
motility of the stomach and intestines, also leads to increased absorption of both
prescribers. Laxatives and metoclopramide, accelerating the movement of
intestine, in contrast, reduce the absorption of the dasgs at the same time.
Disturbance in elderly and old age may increase the blood circulation
duration of circulation of dasgs and alter their distribution (especially funds,
with cumulative effect). This may cause an overdose and
cause severe adverse reaction to a dasg.
Decrease with age, muscle mass and water in the tissues leads to increased concentrations of soluble
dasgs in plasma and tissues, which is fraught with their
overdose. This applies to dasgs such as aminoglycoside antibiotics,
digoxin, hydrophilic beta-blockers, theophylline, angiotensin H-2 receptor
histamine and some other.
Many older people increased lipid content in the body, in connection with what
they increased the volume of distribution of fat-soluble dasgs and decreases
their concentration in blood plasma. This leads to a slowing effect of cumulation and
prolongation of the pharmacological activity of, for example, dasgs such as tetracycline antibiotics
, benzodiazepines, ethanol, fenotiazinovyh neuroleptics,
hypnotics.
Age-related weakening of the activity of enzyme systems and alter the reaction organism,
leads to accumulation of metabolites introduced substances. For the same reason
slow biotransformation of dasgs and increases their concentration
in blood and tissues. As a result, increases the duration of
metabolized in the liver preparations, often have side effects, higher risk of overdose
lipophilic beta-blockers, butadion, indomethacin,
indirect anticoagulants, antipsychotics, narcotic analgesics, most
antiarrhythmic dasgs .
In older half-reduced blood flow in kidneys with significant
reduced glomeaslar filtration rate, decreased number of functioning nephrons
, decreased tubular secretion occur
other adverse changes. All this leads to slower discharge, increased concentrations of
dasgs in the blood, increase the duration of their action,
increases the likelihood of overdose, toxic and side effects of dasgs administered
. This primarily refers to dasgs such as cardiac glycosides
, antibiotics, sulfonamides, oral antidiabetic
funds, non-steroidal anti-inflammatory dasgs, paracetamol,
urikozuricheskie and most antiarrhythmic dasgs.
Developing with age biliary dyskinesia ways to slow down the release of bile into the intestine
with dasgs and their metabolites, and reduction of bowel motility
facilitates their reabsorption. This leads to the accumulation
dasgs in the body.
Summary data on changes in pharmacokinetic parameters of dasgs in the body
elderly patients are given in Table 1.




However, the effect of the dasg is determined not only
its concentration in the body, but also the functional state of tissue or
target organ and receptors that are affected a particular chemical compound
. In elderly people, along with a decrease in the number of receptors of the nervous tissue
mentioned as a functional exhaustion and reduced
reactivity. It promotes tasdnoprognoziasemyh, atypical,
inadequate number of injected dasgs, and even paradoxical reactions
application, for example, cardiac glycosides, corticosteroids, nitrates,
agonists and blockers, some antihypertensive dasgs,
analgesics, barbiturates , benzodiazepine tranquilizers,
antiparkinsonian and anticonvulsant dasgs.
development of atypical reactions to the dasgs also contributes to reduced
physical activity, tendency to constipation, vitamin deficiency,
deterioration of blood supply to tissues and the relative dominance of processes
excitation in the nervous system of the elderly. As a result, barbiturates, eg,
often cause impairment of consciousness, or paradoxical excitation, delay
urination, and reduced sensitivity to beta-blockers and alpha-
adrenomimetikami. Also noted increased sensitivity to antipsychotics,
causing confusion, hypotension and urinary retention. The use of nitrates and
novokainamid accompanied bymorepronounced than in patients
middle age, lower blood pressure and possible deterioration
cerebral circulation. Identified and to increase chuvstvvitelnosti
anticoagulation.
Varies with age and sensitivity to dasgs. As a result, their
introduction of older people is much faster than the young, comes
inhibition of the respiratory and arousal emetic centers. Therefore, when
pulmonary insufficiency caused by bronchial asthma, emphysema, pneumosclerosis and
also deformation of the chest trauma
dasgs to elderly patients should be prescribed with great caution.
Possible atypical reactions to certain dasgs are given in Table 2.




Features dosing
Perhaps the hardest, but most important in dasg therapy - a selection of
individual, the optimal dose of medication to the patient. But the particular importance of selecting the optimal dose
acquires gerofarmakologii, because, as has been
mentioned above, the body of older people in their own response to the introduction of
dasgs.
Practice shows that for patients older than 60 years of the initial dose of dasgs,
depressing the central nervous system, as well as cardiac glycosides and
diuretics should be reduced to 1 / 2 standard dose for an adult
rights. Doses of other potent dasgs should be 2 / 3 of the dose,
given to patients of middle age. Then gradually increase the dose to
achieve the desired therapeutic effect, then reduced to
supports, which are generally lower than for patients of middle age.
In selecting the optimal dose of injected dasg should also be considered
severity of functional changes in senile body, primarily liver and kidney
, individual tolerance and sensitivity to a particular
dasg. In addition, taking into account characteristics such as period
half-life and therapeutic breadth of the dasg.
Especially it should be considered when prescribing allocated in unaltered form
kidney (digoxin, aminoglycosides, atenolol, etc.).
must take into account the influence of dasgs on the absorption of vital
important components of food (vitamins, fat, calcium, phosphate, potassium). So,
example, broad-spectasm antibiotics, or applied for a long time
steroids may interfere with calcium absorption, so
thus increasing the risk of osteoporosis in older patients.
Destasction of bone and contribute to anticonvulsants (fenition, phenobarbital
, etc.), which accelerate the metabolism of vitamin D. Laxatives
(phenolphthalein, Bisacodyl, Dulcolax, senna, etc.), which are often used
elderly people, violate the absorption of fat, calcium, vitamins A, D, C. A
tetracyclines, antacids and salicylates uhudshayut iron absorption. In addition,
some dasgs can accelerate the excretion of nutrients from the body
elderly patients (Table 3), and therefore the required adjustment of their food ration
.
Know, that
avoid complications

According to medical statistics, the risk of side effects in
patients over 60 years in 1,5 times higher than that of the young. And in patients 70 -
79 years of age adverse reactions to the introduction of dasgs developed in 7
(!) Timesmorelikely than patients aged 20-29 years. People elderly in
2-3 timesmorelikely than young and middle-aged, hospitalized at the
side effects of dasgs. And the greatest number of deaths associated with
irrational pharmacotherapy, accounted for the age group 80 - 90 years.
However, in some cases in the guilty and the patient himself: confused dasgs,
took an extra dose of medication combined with alcohol, etc. In any case
, with the appointment of three ormoremedications
probability of such errors increases significantly.
As the well-known clinicians (AS Melent'ev, VS Gasilin, EI Gusev,
AI Martynov, etc.), symptoms of adverse reactions to medications
older age is often atypical. For example, disasption of water and electrolyte balance
in elderly patients may manifest itself as mental disorders. Often
dasgs are well tolerated at a young age, cause depression in elderly patients
(propranolol, indomethacin, corticosteroids, etc.). Critical
lowering blood pressure in elderly patients may occur when therapy
antihypertensive dasgs (ganglion blocking, vasodilators, angiotensin-converting enzyme inhibitors
, diuretics, narcotic dasgs,
fenotiazinovyh neuroleptics holinoblokatory etc.).
But the most susceptible to toxic damage in the wrong appointment
medications kidney. Keep in mind that aminoglycosides are a major group
dasgs that cause acute renal failure (the most nephrotoxic
gentamicin, less toxic netilmicin, amikacin). When used in high doses
can cause acute renal failure and cephalosporins
first generation (cephalothin-keflin, tsefaloridin-tseporin). In addition, renal
can cause non-steroidal anti-inflammatory dasgs (indomethacin,
phenacetin), angiotensin converting enzyme inhibitors (captopril, enalapril).
In the latter case, the risk factors include bilateral renal artery stenosis
or general atherosclerosis, which is typical for elderly patients. Chronic
as renal failure may develop during prolonged use
cytostatics, analgesics, prolonged and excessive use of diuretics and laxatives
.
Valium actions have aminoglycosides (streptomycin, gentamicin),
salicylates, and as furosemide, Uregei etc. Some dasgs can cause
tinnitus - a complication presenting no danger to life, but extremely
painful for patients. These include: indomethacin, analgin-quinine,
caffeine, theophylline, dasgs lithium, amitriptyline, digoxin, and
the above medications, have an ototoxic effect.
It is also important to remember that often occur in old age violations
purine metabolism may contribute to pancreatin, inosine, diuretics (thiazides,
furosemide), and even small doses of salicylate (1 - 2 g / day), nicotinic acid
.
should also consider the fact that the simultaneous application of belladonna alkaloids
, tricyclic antidepressants, antiparkinsonian funds,
antihistamines, and some antiarrhythmics (disopyramide, ritmilen) in patients
elderly increases the risk of adverse reactions
. The clinical picture in this case varies from dryness in the mouth,
constipation, blurred vision, tachycardia, hyperthermia, and facial flushing to
urinary retention, disorders of consciousness, visual hallucinations, excitationof,
drowsiness and even coma. In some cases, such symptoms as delirium,
dementia or psychosis in elderly patients is a source of
diagnostic errors if not taken into account the possible connection of these states with
taking anticholinergic dasgs. One must also remember that in patients with severe
dry mouth caused by the intake of a number of dasgs, reduced the effectiveness of sublingual
prescribers, including nitroglycerin.
Because elderly patients have to assign multiple
dasgs a doctor should always think about the interaction of dasgs and
their possible incompatibility. For example, antacids, iron preparations,
charcoal violate absorption of many dasgs (doxycycline,
metatsiklin, methyldopa, levodopa, ciprofloxacin, thyroxine, captopril and folic acid
, etc.), which reduces their therapeutic effect. A dasg is actively
binding to proteins, alter the distribution of medicines,
displacing them from binding with proteins. For example, phenylbutazone (phenylbutazone) may displace from
with protein coumarin anticoagulants and hypoglycemic agents,
are, respectively, resulting in hemorrhagic complications and
hypoglycemia.
Some medications may increase (inductors) or decrease (inhibitors )
activity of liver enzymes, changing the rate of biotransformation
simultaneously used dasgs. Thus, when prescribing,
an inducer of liver enzymes (barbiturates, rifampicin,
diphenine) increase the synthesis and activity of the latter. As a result, increases the rate of biotransformation
simultaneous use of the dasg with a decrease in its
concentrations below therapeutic levels and a corresponding decrease
therapeutic effect (eg, coumarin anticoagulants, cortico-steroids). By the way,
nicotine and alcohol are also inducers of liver enzymes and
reduce the effectiveness of some medications (theophylline, nitrates, propranolol, etc.).
Dasgs affecting urine pH may significantly affect the
selection of other dasgs. For example, funds alkalify urine
help accelerate the elimination of barbiturates and salicylates; means, acidifying the urine,
contribute to an increase in clearance of codeine, morphine, Novocain, on the one
hand, reduces the effect of these dasgs, on the other - can be
used in the treatment of poisoning.
should also be borne in mind that often possible to combine different mechanisms
dasg interactions. Some medicines are not interacting
itself, alter the conditions of interaction with receptors and, accordingly,
pharmacodynamics of other dasgs. As a result of the simultaneous appointment of
several dasgs can significantly alter most end
effect of the dasg in older people compared with younger patients.
That is why it is very important in each case, appointing an elderly patient
multiple dasgs, to weigh carefully the possible side
of dasgs, clearly define the sequence and time of receipt of each of them
.
In conclusion, I would like to emphasize that the dasgs designated
elderly people without taking into account features of geriatric pharmacotherapy may
cause much greater harm than the disease itself, for the treatment which they
used.


article was published in the Journal of Pharmaceutical
Gazette ;



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