AUTONOMIC DRUGS
Autonomous medications are drugs that can affect the channeling of impulses in SSO with the way interfere with the synthesis, accumulation, acquisition, or the breakdown of neurotransmitters or affect his work on special resptor. The result is smooth muscle and affects the function of organs, heart and glands. There are 2 kinds of autonomic drug classes namely, Class sympathomimetic (stimulating), which works similar to the sympathetic nerve, and Group simpatolitik (inhibit) for the sympathetic and parasimpatolitik. According to the properties, autonomic drugs can be classified as follows:
1. Substances that work against SO, namely:
a. Simpatomimetika (adrenergika), which mimics the effect and SO stimulation by eg noradrenaline, ephedrine, isoprenalin, and amphetamines.
b. Simpatolitika (adrenolitika), which suppress or counteract the effects of sympathetic nerve adrenergika. eg alkaloids sekale and propranolol.
2. Substances that work against the SP, namely:
a. Parasimpatikomimetika (kolinergika) which stimulate the organs that are served and mimic the effects of parasympathetic nerve stimulation by acetylcholine, for example Pilocarpine and fisostigmin.
b. Parasimpatikolitika (antikolinergika) precisely against kilonergika effects, such as alkaloids, Belladona and propantelin.
3. Stranglehold substances ganglion
Which impedes forward impulse in the sympathetic ganglion cells and the parasympathetic. This counteraction effect broad impact, such as vasodilatation due to sympathetic blockade arrangement, so that is used in particular hypertension. As a hypertension drug substances are generally not used anymore related side effects that cause blockade also from SP (impaired vision, obstipasi and reduced secretion of various glands).
1. DRUG SYMPATOMIMETIK / ADRENERGIKA
Is a drug that facilitate or mimic some or all of the actions of the sympathetic nervous system. Adrenergika drug is also substances that can cause the same effect as the sympathetic nervous system stimulation and noradrenaline release in nerve endings. Substances with effects that actually inhibit the central-adrenergic system, for example klonidin, excluding adrenergika. Organism prepared so quickly to produce a lot of energy, which is ready for a reaction of "fight, Fright, or flight" (a fight, feel scared or run away). Therefore adrenergika has a power that aims to achieve the state of alert.
a. Receptor alpha and beta
Adrenergika can be divided into two groups according to work points on effector cells of end organs, namely receptor-alpha and-beta receptors. The difference between these two types of receptors based on their sensitivity to adrenaline, noradrenaline and isoprenalin.
Further differentiation can be made according to physiological effects, namely the alpha-1 and alpha-2, and beta-1 and beta-2. In general, each of stimulation of receptors that produce effects as follows:
v Alpha-1: cause vasoconstriction of smooth muscle cells and stimulating the gland by increasing the secretion of saliva and sweat.
Alpha v-2: inhibits the release of NA in the adrenergic nerves to the decrease in blood pressure. Munkin release of ACh in nerve kolinergis in the intestine also inhibited so decreasing peristaltic.
v Beta-1: strengthening the power and frequency of heart contractions (inotrop effects and katrotop)
v Beta-2: bronchodilatasi and stimulation of glycogen and fat metabolism.
b. Mechanism of action
Katecholamin worked as a "lackey" (transmitter) and bind themselves to receptors located in the outer membranes of cells. Merger is activate an enzyme inside the cell membrane to increase the conversion of adenosine thiphosphate. ATP is rich in energy, which was released on pengubahannya into cAMP in the cell, mangakibatkan various adrenergic effects.
c. Classification
Adrenergika can be divided into two groups, namely:
· Substances that work directly, most katecholamin work directly against the goal of the organ receptors, such as adrenaline, NA and isoprenalin. Known also by substances that can work according to two principles, such as ephedrine and dopamine.
· Substances that work indirectly, noradrenaline is synthesized and stored in adrenergic nerve endings and can be freed from depotnya by stimulating the nerve in question, and can also with the mediation of drugs such as ephedrine, amphetamines, guanetidin, and reserpin.
d. Use
Based on these properties, adrenergika used in a variety of diseases and disorders, the most important are:
· In shock in order to strengthen the heart and against hypotension, particularly adrenaline and NA
· In order to achieve bronchodilatasi asthma, especially salbutanol and its derivatives, as well as adrenaline and ephedrine.
· In order to reduce the hypertension-resistant peripheral artery wall by inhibiting the release of NA. besides that, also through the blockade resptor and (prazosin / propanolol and its derivatives)
· As peripheral vasodilators on dibetis vasoconstriction and leg.
· On a cold (rhinitis) in order to shrink the swollen mucosa, especially imidazolin substances, also rarely ephedrine and adrenaline.
· As midriatikum in order to dilate the pupil, such as phenylephrine and nafazolin.
· In obesity in order to suppress appetite to support diets attenuate body, especially fenfluramin and mazindol.
· As his blocks and on menstrual pain, thanks to the relaxation of the muscles of the uterus, for example ritodrin.
e. Side effects
In normal doses, adrenergika can cause side effects on the heart and CNS, namely tachycardia and palpitations, headache, anxiety and so forth. Therefore, adrenergika should be used with caution in patients who suffered from myocardial infarction, hypertension and hipertirosis.
When used long as in asthma, adrenergic bias caused tachyfylaxis, a kind of resistance which occurs rapidly when the drug is given repeatedly in a short time. The best known is ephedrine and other drugs with indirect employment due to endless supply of NA. Therefore, these drugs should not be used continuously, but interspersed with other asthma medications.
f. Separate substances
A. Epinephrine: This substance is produced also by the children's kidneys and role in carbohydrate and fat metabolism. Adrenaline has all the properties of adrenergic-alpha and-beta, but beta relatrif stronger effect.
Its use, particularly as a heart stimulant drug analepticum that is active at all in an emergency, such as collapse, shock anafilaktis, or the heart stops. These drugs are very effective for acute asthma attacks, but should be as outlined by injection Because peroral gastric juice. In particular glaucoma is used to lower intraocular pressure. This effect before very paradoxical, because the adrenaline antagonist widely used to lower the same indication.
The side effects are important at high doses is the radius of necrosis due to vasoconstriction and eventually collapse.
Dosage: In acute asthma s.c. 0.2 to 0.5 mg, if necessary, repeated twice every 20 minutes, max 1 mg each time. At the heart stops / bradycardia, shock anafilaktis im 0.5 mg, followed by i.v. 0.5 to 1.0 mg, if necessary, repeated every 2-5menit. Terbuka1 glaucoma drops 2-5 mg / ml.
B. Norephinephrine
Pharmacological effects:
1. Most of α affects when given a treatment which is contrary to the expected results endrogin that adrenergic neurotransmitters have vasoconstriction around.
2. The increase in diastolic blood dipembuluh and systolic.
3. Reflex bradycardia
Indications norephinephrine:
1. Shock due to blood flow in obstructed kidney
2. Treatment with dopamine is better to first aid.
Various kinds of drugs ephinephrine namely:
1. Isoprenalin: isoproterenol, isoprel, lomudal cp.
Homologous adrenaline is primarily a β effect (stimulation of the heart and broncodilatasi), now exclusively used in asthma and as a stimulant of blood circulation. Pentakaran more closely achieved through aerosol (spray) with long working approximately 1hr. Spray should not be repeated too often so as not to cause an overdose.
Side effects mainly occurred in high dose and form of cardiac effects and central effects (anxiety, fear, difficulty sleeping) was also shaking and so on.
Dose: 0.08 to 0.4 mg at a maximum of 8 bronchospasme inhalation solution sulfate 1% a day, to improve circulation iv the beginning of 0.02 mg, followed by 0.01 to 0.2 mg.
2. Phenylephrine: Prefrin, Benadryl DMP, Vibrocil.
These drugs are particularly vulnerable alpha-adrenergis indirectly by liberation of NA from nerve endings. These drugs act about 10 times weaker than the adrenaline, but last longer. Not stimulate the CNS, the effects of mild heart once.
Another use is as midriatikum on eye examination (5-10% chloride solution) that starts after 20 minutes and bias persist for 7 hours. Besides used dekongestivum nose and eye (0.125 to 0.5% solution).
As a side effect noted among other soft contact lens refractive dark brown. Because entry into the milk by cause hypertension in infants, the mothers who breast-feeding is not recommended to use eye drops with this substance.
3. Ephedrine: Asmasolon, Bronchicum.
These drugs act on the CNS relative to the heart stronger and last longer. In addition to working directly on the receptors in smooth muscle and heart, as well as indirectly to release NA from depotnya.
Its main usage is in asthma due to the effects of strong bronchodilatasi (β2), as decongestivum and midriatikum less stimulating than the adrenaline.
The side effects at normal doses are uncommon central effects such as restlessness, headache, anxiety and difficulty sleeping, while in the overdose resulting tremors and tachycardia, arrhythmia and heart pounding. Pregnant women may use ephedrine.
Dose: in asthma 25-50 mg 3-4 dd (-HCL), children 2-3 mg / kg daily in 4-6 doses. Sulfate solution nose drops from 0.5 to 2%, 3-4% in eye drops.
4. Amphetamines
Amphetamines including psikostimulansia group characterized by stimulating the central nervous system and strengthen the respiratory inhibited by other central drugs. Physical and mental activity increases, so does the initiative and agility. Self-confidence and achievement is enlarged, whereas drowsiness and fatigue are removed (temporarily). Amphetamines also cause a sense of comfort / then based on the nature of this psychic was used as an antidepressant. In addition it also has the effect of adrenergic amphetamines which include vasoconstriction, bronchodilatasi, midriasis, and contraction of the bladder sphincter.
2. DRUG SIMPATOLITIK / ADRENOLITIKA
Are substances that resist most or all of the activity of the sympathetic nervous system. For example, adrenolitika negate that in vasoconstriction caused by activation of receptor-alpha due to adrenergika. Based on the mechanism and point it works, adrenolitika can be divided into three groups, namely oxygen-adrenergic receptor inhibitor (alpha-blockers and beta-blockers) and substances inhibiting adrenergic neurons.
1. Alpha-blockers (α-simpatolitika)
These substances block the receptor-alpha are numerous in the smooth muscle tissue of most vessels, especially in vessels of skin and mucosa. Its main effect is peripheral vasodilatation, it is widely used hypertension and prostatic hypertrophy. Prazosin also used in heart failure. Known three types of alpha-blockers, namely:
- No selective agents: fentolamin and ergot alkaloids.
Fentolamin specially used for diagnosis and therapy of certain hypertension. Also on erection problems as injection intracaverneus. Ergot alkaloids, thanks to the power vasokontriksinya widely used in migraine attacks, as well as in obstetrics to stop the bleeding after childbirth.
- Selective α1-blockers: derivate quinazolin (prazosin, terazosin, tamsulosin, etc.) and urapidil. Its use as a medicine in hypertension and prostate hyperplasia.
- Α2-selective blockers: yohimbine, which is used as the passion of stimulant drugs (aphrodisiacum).
2. Beta-blockers (β-simpatolitika)
Originally beta-blockers used for heart problems. To alleviate this organ sensitivity to stimuli, such as heavy work, emotion, stress, and so forth. These medications can also be divided into 2 groups, namely:
- Β1 selective agents, which counteract the effects of stimulation by adrenaline and NA jntung (receptor-β1), such as atenolol and metoprolol.
- No selective agents, which also inhibits the effects bronchodilatasi (receptor-β2), such as propranolol, alprenolol etc.
- Labetolol and carvedilol are substances that inhibit both receptors (alpha + beta)
3. Adrenergic neuron inhibitors: guanidine derivate (guanetidin).
These substances do not block the receptor but rather to work towards the postganglioner from sympathetic nerves by preventing the release of katecholamin. Special Guanetidin used on certain types of glaucoma.
a. Separate substances
Yohimbine
This alkaloid derived from yohimbe bark corynanthe (west Africa). The bark also contains other alkaloids, namely aspidospermin.
In low doses can increase blood pressure, whereas at higher doses it down. Therefore, peripheral vasodilation occurs resulting in enhanced blood supply to the organs in the lower abdomen.
Side effects may include decreased blood pressure, dizziness, sweating, strong, heartbeat, tremor, agitation, anxiety and difficulty sleeping, seizures bronchi and lupus-like symptoms. In people with mental disorders, low doses can trigger depression.
Dose: 5-10 mg orally 3-4 dd.
3. PARASYMPATIKOMIMETIKA / cholinergic
Is a group of substances that can cause the same effect as the composition of parasympathetic stimulation (SP), because neurohormon release of acetylcholine (Ach) at the ends of neurons. SP main task is to collect energy from the food and prevent its use, simply serves as assimilation. When the neuron is stimulated SP, timbulah a number of effects that resemble a state of rest and sleep.
a a. Classification
Kolinergika can be divided according to how it works, ie substances with direct employment and working substances indirectly.
1. works directly: karbachol, Pilocarpine, muskarin, and arekolin. These substances work directly to the organ-end with similar major work muskarin effects of ACh. Everything is kwaterner ammonium substances which are hydrophilic and difficult to enter the CNS unless arekolin.
2. Indirect work: Anticholinesterase substances such as fisostigmin, Prostigmin and pyridostigmin. These drugs inhibit the breakdown of ACh in a reversible, that is only temporarily. After tersebuthabis substances described by cholinesterase, ACh soon be overhauled again.
b. Use
Special Kolinergika used in eye disease glaucoma, myasthenia gravis, Alzheimer's dementia and atonia.
1. glaucoma
green star (glaucoma) is an eye disease characterized by an increase in intraocular eye fluid above 21 mm Hg, which can clamp the optic nerve. Cause, eye fluid formed in the thin mucosa behind the pupil, in the corpus ciliare and via hole pupil flows into a narrow space between the pupil and cornea to the channel exit. When this fluid can not flow out of the front eye chamber because such a blockage, then the eyes of intraocular fluid increases.
2. Myasthenia gravis
This is an auto-immune disease characterized by fatigue and weakness of muscles, especially the face, eyes and mouth. The reason is the relative lack of ACh at the motor end plate of striated muscle. This deficiency is caused by IgG antibodies, which have damaged the local ACh receptors.
3. Alzheimer's Dementia
Based on the discovery that reduced brain ACh levels in dementia, the cholinesterase inhibitors used to prevent reform and improve the levels of ACh in the brain.
4. atonia
after major surgery with stress to the body sometimes an increase in adrenergic nerve activity. The result can be obstipasi and difficult urination, and even intestinal obstruction due to relaxation and peristaltic paralysis.
c. Side effects
Kolinergika Side effects are similar to the effects of SP stimulation in excess, such as nausea, vomiting and diarrhea, as well as increased secretion of saliva, sputum sweat and tears.
4. PARASYMPATIKOLITIKA / ANTIKOLINERGIKA
Parasimpatolitika Antikolinergika or against the efficacy of acetylcholine by inhibiting primarily muskarin receptors located in CNS and peripheral organs. These substances do not work on nicotine receptors except ammonium kwartener substances are powerless against him lightly.
Most antikolinergika not work for five selective receptor subtype-M. effect on many organs, among others; eyes, exocrine gland, lung, heart, urinary tract, gastrointestinal tract, and CNS.
a. Classification
Antikolinergika can be divided into 3 groups, namely:
1. belladonna alkaloids: atropine, hyoscyamin, scopolamine and homatropin
2. ammonium substances kwartener: propantelin, ipratopium and tiotropium
3. tertiary amine substances: pirenzepin, flavoxat, oksibutinin, tolterodin and tropicamida.
b. Use
Depending on the specific nature of each, antikolinergika used in pharmacotherapy for various disorders, the most important are:
1. as midriatikum, to dilate the pupil and paralyze accommodation (atropine, homatropin, tropikamida)
2. as spasmolitikum (muscle cramp reliever) from the gastrointestinal tract, biliary tract and urogenital organs.
3. on the bladder instabil inkontinensiurin result of detrusor muscle hyperactivity.
4. as an anti-drunk way, in order to prevent nausea and vomiting (scopolamine)
c. Side effects
of the effects of dry mouth muskarin ie, obstipasi, urinary retention, tachycardia, palpitations and arrhythmia, impaired accommodation, midriasis and sweating. At high doses arising central effects, such as anxiety, confusion, and hallucinations.
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