ANTI-DEPRESSANTS- SEROTONIN SPECIFIC RECEPTOR INHIBITORS- S.S.R.Is

 WHAT ARE SSRIs?

Fig-1
SSR-Serotonin Specific Reuptakereceptor
DSR-Dopamine Specific Reuptakereceptors
NSR-Noradrenaline Specific Reuptakereceptor
SSRIs specifically block the reuptake of serotonin only and make it available in the synapse while other hormones are reuptake by their receptors and disappear from the synapse as shown in the Fig-1 (3)

Serotonin is the key hormone of the central nervous system that stabilizes our mood, feeling of peace, and pleasure. In a single term, it is the 'Hormone of Peace and Pleasure'

Medical science has categorised this hormone as a CNS inhibitory hormone but this hormone bears stimulant effects also to some extend such as regulating communications between the brain cells and other nervous system cells. This hormone helps the body with sleeping, eating and digestion. 

Serotonin helps the body with sleeping is by its CNS inhibitory effects. Serotonin when compared with GABA helps the body to sleep normally with healthy and natural sleep while GABA and GABAergic drugs produce unhealthy and addictive sleep. Most of the sleeping pills belong to the GABAergic category.

Similarly, serotonin helps the mind to relieve depression is by its CNS stimulatory effects. Serotonin when compared with other CNS stimulants like noradrenaline, and dopamine helps the mind to get out of the blues with minimal side effects.

That is why S.S.R.Is are considered to be safer than other tricyclic antidepressants like amitriptyline, nortriptyline and protriptyline.

S.S.R.Is are the most preferred medicines to alleviate Obsessive and Compulsive Disorder (O.C.D).

There are many S.S.R.Is are available and dispensed at the pharmacy on Doctor's Prescription only. They are,

1.Fluoxetine (Prozac); 

2.Sertraline (Zoloft);

3.Paroxetine(Paxil);

4.Fluvoxamine(Luvox)

The following two drugs are newer members included in this group.

1.Citalopram (Feliz)

2.Escitalopram (Nexito)

Many more new chemicals are coming up with attractive names in this category.

It is not the purpose of this article to describe them all in detail.

One thing is very important to note that in English Medical System (Allopathy) 'minimum side effects of drugs are not yet well defined'

These drugs can be mentioned as one of the many examples of this.

Take a look at a miracle that the same Allopathy Medical Science lists below as to what effects these drugs, which are advertised as having minimal side effects, can cause when used incorrectly and over a long period of time.

The followings are the 'minimal side effects when compared ' with other antidepressants:-

1.Anticholinergic effects-blurred vision, constipation, dry mouth, urinary retention.

2.Antihistaminic effects- low B.P, elevated heartbeats, mucus thickening and airway block, difficulty urinating and constipation.

3.α-adrenergic blockade-palpitations, tremor, anxiety and hypertension.

The followings are the actual side effects of SSRIs:-

1.Nausea, diarrhoea

2.Nervousness

3.Difficult to sleep or sleeplessness

4.Dizziness

5.Impotence and decreased desire for sex

PRECAUTION:-More dangerous than all this is 'serotonin syndrome '. Very dangerous. That taking these SSRIs inadvertently with any MAOI antidepressants such as selegiline (Eldepryl, Zelepar), isocarboxazid (Marplan), Phenelzine (Nardil), tranylcypromine (Parnate).

The characters of serotonin syndrome are,

1.Hyperthermia-Elevated body temperature

2.Muscle rigidity-Paralysis

3.Myoclonic seizures

4.Disturbances of mental status.

Natural Healthyway to improve serotonin

Tryptophan is one of the nine essential amino acids

needed by the body through foods. 

Serotonin is nothing but 5-hydroxytryptophan.

Any food that is rich in tryptophan can improve the availability of sufficient serotonin at the CNS nerve synapses.

Foods that are rich in tryptophan are,

1.Chocolates

2.Oats

3.Dried dates

4.Milk and dairy products

5.Mutton, beef and eggs

6.Fish

to see further click here

But if you desire to take foods that are high in tryptophan then you should first stop taking the SSRIs, MAOIs and Tricyclic antidepressant drugs completely with your doctor's guidance

Conclusively do not go to psychiatric medication to get out of your mental blues instead go to s clinical psychologist and get good counselling from him.

DO SLEEPING PILLS DAMAGE KIDNEYS?

 RHABDOMYOLYSIS AND KIDNEY DAMAGE

Fig-1
To have a clear look please click on the figure

Rhabdomyolysis is a rare but potentially life-threatening disease resulting from the disintegration of skeletal muscle cells (myocytes) with the leakage of toxic muscle cell contents into the extracellular space and blood circulation.

The major causes for this condition are direct muscle injuries by accidents, chronic myalgia, myopathies and indirect muscle injuries by immobilization in a place for a long time during a flight journey, or in a car, overexertion, heavy exercises, and drug abuse like HMG Co-A Reductase Inhibitors (...statins), narcotics, sleeping medicines, antihistamines, anticholinergics, amphetamine, alcohol and cocaine.

Narcotics and sedatives like sleeping pills cause indirect heavy pressure into the striated muscles to cause muscle damages.

Common OTC antihistamines such as doxylamine and diphenhydramine are available freely at the pharmacy counters. Prolonged use can cause myopathies.

Diet supplements or weight loss supplements that contain creatine and ephedra a plant that contains non-selective adrenergic agonist ephedrine (Anticholinergic) can cause this deadly disease.

Anticholinergics, antihistamines anxiolytics and sedatives cause heavy pressure on the striated skeletal muscles in the body in some parts or as a whole that may lead to muscle fibre damages.

Prolonged use of statins like simvastatin and rosuvastatin can cause rhabdomyolysis, especially with low serum vitamin D (<10ng/ml). Anybody take statin medicines for a long time must include vitamin -D in their prescription.

Heatstroke and overexertion cause muscular cell damages that lead to rhabdo.

Hypothermia in which the body temperature drop can produce many complications such as cardiovascular and neuronal defects that may exert heavy injury in the skeletal muscles. Avoid prolonged exposure of your body in extremely cold weather, and do not immerse your body in ice-cold water for a long time.

Viral and bacterial blood infections that are injurious to your muscle fibres.

Electrolytes such as potassium and calcium irregularities.

Hypothyroidism and hyperthyroidism

Kidney disorders elevate myoglobin in the blood.

Surgery that causes prolonged bed rest and immobilization that causes skeletal muscle disintegration.

Sickle cell anaemia

prolonged muscle inflammations.

Among all the above-mentioned causes for rhabdomyolysis, some are non-traumatic drug-induced indirect skeletal muscle injuries.

In rhabdomyolysis, there are elevations of serum myoglobin and creatine phosphokinase (CPK) in the blood followed by myoglobinuria in the urine.

Elevated CK cause hypotension and low blood supply to various organs like the kidney and the liver that leads to multiple organ failure.

Elevated CK also causes Compartment Syndrome.

SUMMARY OF CAUSES IN BRIEF

1.Muscle injury by accidents

2.Pressure on the muscles due to long time immobilization such as prolonged bed rest, long journey, coma.

3.Abusive drugs, such as narcotics, sedatives, antipsychotics, and antidepressants.

4.Prolonged and untreated burn injures.

5.Vitamin -D deficiency

6.Prolonged untreated microbial infections, skin cancers, psoriasis which damage skeletal muscles can precipitate rhabdomyolysis.

7.Prolonged body exposure to ultraviolet rays, harmful chemicals can cause rhabdomyolysis.

8.Overdosage and prolonged use of ...statin drugs like simvastatin, atorvastatin and pravastatin.

If you have acute or chronic pain in your lower back or neck and you are using narcotics, sedatives such as sleeping pills or any other psycho drugs and passing urine by dark red or brown colour, that confirms rhabdomyolysis. (See Fig.2)

Fig-2

Blood Profile in Rhabdo

1.Elevated muscle enzymes such as creatine phosphokinase (CPK), SGOT, SGPT, and LDH.

CPK level rise in the blood above 1000 U/L. That is 5 times the upper limit normally indicate rhabdomyolysis.

Myoglobin level exceeds 1.5mg/dl  

Too much intake of protein with heavy exercise may elevate CPK level in the blood.

Urine Profile in Rhabdo

Colour =  Dark Pinkish Red or Dark Brown

Creatine Phosphokinase (CPK) = Above 1000U/L

Myoglobin = even traces in the urine can indicate the presence of rhabdo but the colour of the urine changes to dark red or brown when myoglobin exceeds above 100gm/dl.

Fig-3

Any kind of muscular abuse can result in myalgia, myositis and rhabdomyolysis. These abuses are traumatic, or by drug overuses or by infections.

All antipsychotics including sleeping medicines, anticholinergics, antihistamines, are prone to abuse your muscles.

Symptoms of Rhabdo:

1.Muscle pain in the shoulders, thighs, or lower back.

2.Muscle weakness

3.Trouble moving arms and legs

4.Dark brown or red urine.

5.Decreased urination.

6.Abdominal pain

7.Nausea, vomiting

8.Fever, hyperthermia

9.Tachyarrhythmia

10.Confusion, and dehydration.

Sleeping Medicines That Causes Indirect Non-Traumatic Skeletal Muscle Injuries:

1.Alprazolam

2.Diazepam

3.Clonazepam

4.Lorazepam

and many other benzodiazepines.

5.Barbiturates

6.Opioids like heroin, morphine, codeine.

7.Abusive narcotics like cocaine, heroin, LSD, ketamine

8.Alcohol

Diagnosis:-

The most reliable diagnostic test for rhabdomyolysis is the elevated level of creatine phosphokinase(CPK) in the blood that is above 1000mg/dl.

This followed by a myoglobin test in the urine (dark pink coloured) test that confirms rhabdo.

Rhabdo-Treatments at Home:

The following home remedies can be beneficial when the disease is at the beginning stage.

1.Rest and relax conveniently so that muscle can recover from the damage.

2.Take plenty of water, light broth and sports drink to rehydrate your body and to prevent further kidney damages.

3.Withdraw abusive drugs such as sleeping pills step by step under the doctor's supervision.

4.Completely stop taking...statin like cholesterol-lowering drugs. 

5.Stop performing hard and heavy exercises.

6. If you feel tired recline in comfort and relax.

Compartment Syndrome

Fig-4
Lower Extremity Compartment Syndrome

Severe rhabdomyolysis at the extreme stage that may develop after fluid resuscitation produces potential complication like Compartment Syndrome.

Our body skeleton and skeletal muscles are divided into many compartments which are covered and separated by a special thick membrane known as Fascia.

Every compartment is supplied with muscle fibre cells, extra and intracellular fluids and components, neuronal and supplies. Any injuries to the myocytes, directly and indirectly, will disturb this system in a compartment, causes fluid collection inflammation and oedema in that compartment will lead to rhabdomyolysis.

Complications of Rhabdomyolysis:

1.Increased blood clotting

2.Low Pressure

3.Shock

4.Kidney and liver failure due to necrosis and insufficient blood supply.

5.Electrolytic imbalance.

6.Hypoalbuminemia (Blood albumin depletion)

7.Hyperuricemia (Increased uric acid level in the blood)

8.Compartment Syndrome

9.Disseminated Intravascular Coagulation. (DIC)

Disseminated Intravascular Coagulation. (DIC)

DIC is a condition affecting the blood's ability to coagulate to stop bleeding.

In DIC abnormal thick clots form inside blood vessels that consume all clotting factors of the blood. The depletion of the clotting factors causes heavy bleeding in all sites of the body.

The major causes of DIC are inflammations, infections, cancers and rhabdomyolysis.

Medical Counselling To Prevent Rhabdo

1. Avoid continuous use of statins and use them at one or two months interval.

2.Systematically withdraw the use of benzodiazepines, barbiturates and any other anxiolytics and sleeping pills.

3.Withdraw step by step the use of any psych medicines like antipsychotics, antidepressants and narcotics like opioids, cocaine, and LSD and completely stop them.

4.Carefully handle antihistamines, anticholinergics,  adrenergic agonists and any other ANS agonists or antagonists under the doctor's advice.

5.Avoid self medications.

6.Do not take anabolic steroid or any other steroid without a doctor's supervisions.

7.Avoid diet control supplements that contain harmful drugs like ephedrine.

8.Be alert when you are taking any hormone drug especially thyroid hormone, androgenic or contraceptive pill.

Non-Medical Counselling

1.Do not perform heavy exercises

2.Do not subject your body to exertion. Be care the job and recreational games that involves exertion, and heat exposure.

3.Drink more water to avoid dehydration before and after strenuous exercises so that your kidneys can eliminate any toxic myoglobin released by your muscle easily.

4.Avoid taking too many proteins and bodybuilders before and after heavy exercises as it may cause elevation of creatine kinase in the blood.

5.Do not sit or stand in one place for a long time.

Conclusively Rhabdo is a rare condition but life-threatening and can occur to anybody at any time without age difference in case if you abuse your body by any means.

SLEEPING PILLS -FEMALE INFERTILITY

 FEMALE INFERTILITY & ABORTION BY REGULAR USE OF SLEEPING PILLS

FIG-1-THE OVARIAN SYSTEM
TO SEE CLEARLY CLICK ON THE FIGURE

Sleeping pills especially benzodiazepines such as alprazolam, diazepam, clonazepam, lorazepam, temazepam, flurazepam, chlordiazepoxide, midazolam, and triazolam cause serious undesirable effects in a female reproductive system such as ectopic pregnancy and abortion.

ECTOPIC PREGNANCY

A team medical study has revealed that regular or chronic uses of benzodiazepines during the period of pregnancy can cause life-threatening conditions such as ectopic pregnancy or abortion.

FIG-2-ECTOPIC PREGNANCY

The benzodiazepines desensitize the movements inside the fallopian tubes thereby block the movements of the fertilized egg and thus prevent it to be implanted inside the uterus. Thus the egg starts the embryonic developments within the fallopian tube to cause ectopic pregnancy. (See fig-2) 

Ectopic Pregnancy(E.P.) is a serious condition in which the fertilized egg is struck within the fallopian tube and begins to develop there. (See Fig-2-above) 

ABORTION, INFERTILITY AND DEFECTIVE BABY FORMATIONS:-

Another study report has revealed that continuous use of benzodiazepines can cause abortion, defective baby development and causes the baby to have a short term addiction to benzodiazepines.

Neuronal hyperpolarization desensitization of the ciliary body blocks the sperm movements into the fallopian tube to reach out the ovum and causes infertility.

Due to the anticholinergic effects of the benzodiazepines the uterine contraction failure leads to cesarian delivery.

Using benzodiazepines in the first trimester may cause cleft lip and palate in the mother and baby. But these risks are small in later stage exposure to alprazolam.

The doctors say diazepam is a safer medication to take during pregnancy but unsafe during lactation. The report continues that chlordiazepoxide is safe during both pregnancy and lactation.

Medical reports suggest that try the antihistamine diphenhydramine (Benadryl) during pregnancy as a safe sleeping aid. But yet all of them are anticholinergics and should be used under the supervision of a licenced medical practitioner.

There are some technical terms in allopathic medication which in practice may not be used to actually what it should be meant for. 

For example, the terms SAFE and SAFER do not mean that the medicine is completely safe or safer but it is with minimal side effects and the minimum in their imaginary scale is a trade secret of the corporate business.

There are many suggestions to use antidepressants such as SSRIs like citalopram, escitalopram or sertraline safely during pregnancy as sleeping aids instead of using traditional sleeping aids. But they have side effects and should be used under expert supervision.

SLEEPING MEDICINE POISONING-SLEEPING PILLS AND MALE INFERTILITY-

 DECREASED LIBIDO BY CONSUMING SLEEPING PILLS

Epididymis 

To view the figure clearly click on the figure

Many studies state that chronic use of sleeping pills like alprazolam, diazepam, and lorazepam can cause hormonal disturbances that lead to male infertility and decreased libido. 

Another study states that chronic use of alprazolam produces pronounced male reproductive defects, especially in testes, epididymis and spermatozoa formation. There are miscarriages and delivery mortalities due to chronic use of benzodiazepine sleeping aids like alprazolam, and diazepam.

Epididymis a coiled tubular structure in which sperm gets matured is severely affected by benzodiazepines said to a study report

Hyperprolactinemia:-

This is one of the major toxicity produced by chronic use of benzodiazepines both in male and female. Benzodiazepines like alprazolam overstimulate the pituitary gland to secrete prolactin which suppresses the normal secretion of Gonadotropic Hormone (GTH or GSH) leads to many sexual dysfunctions both in male and female.

In the male, the following dysfunctions can be observed

1.Decreased testosterone production by the testes

2.Decreased sex drive or libido

3.Male infertility

4.Low sperm count.

5.Epididymis damage

6.Fibrotic and damaged seminiferous tubules, and Leydig cells of the testicles.

Conclusively if you are a young man planning for marriage or a newly married man planning to have a baby please avoid using sleeping pills for a long time.

MEDICAL ERRORS-ANTI-PSYCHOTIC DRUGS

 ANTIPSYCHOTICS OR NEUROLEPTICS

Dopamine Flow in the Brain

Medical errors are substantially increasing in society.

The Erratic Effects of Psychiatric Drugs:-

1.Sleeping Pills (Anxiolytics & Sedatives)↛ Insomnia, parasomnia, somnambulant, anxiety and sedation.

2.Antipsychotics        ↛ Depression, sedation, 

3.Antidepressants       ↛  Excitation, Agitation,&                                                                   Psychosis    All the above can precipitate anticholinergic and extrapyramidal side effect including Parkinson Disease (P.D), Alzheimer's Disease (A.D), panic and sleep disorders etc. etc. 

To have a clear look please click on the figure

Most of them are due to the unawareness of the patients and the non-descriptive drug information by the prescriber and the pharmacist. Antipsychotic drugs are nowadays very commonly taken by the public for years and years. They carry very old prescription to go to the pharmacy and buy the medicines directly from the counter without any restriction and care. They are not aware of the time limit set by their doctor to take the drug. They become an addict to that. They do not revisit the doctor for further opinion on whether to continue the medication or not. This is due to the addiction developed into them. The addictive mind masks the person from taking care of his own health.

All the psychiatric treatments are unrealistic and they do not bring the cure or solution to the problem rather they push the problem further into a deep crisis. (See Fig above).

For example, long use of sleeping medicines to treat insomnia leads to tolerance to produce again insomnia, agitation, and depression. 

Then a long time use of antidepressants leads to agitation and psychoses. 

Then to treat psychosis the patient is asked to take antipsychotics. Prolonged use of antipsychotics leads to again depression. 

The cycle is going without any end and then where is the real cure.

What is Psychosis:-

The Brain 
To see clear please click on the figure

In our Brain System, there are some hormones which are known as brain or central stimulating hormones. They are as follows:-

1.Norepinephrine or Noradrenaline

2.Dopamine

3.Acetylcholine

4.Aspartic acid

5.Glutamic Acid

Out of all the above five, dopamine takes the centre as it is concerned with our mental power of physical movements, memory, motivations and emotional response, reward-motivated behaviour and desire, addiction, hormonal regulations, maternal behaviour (nurturing), pregnancy and sensations.

The 4 Dopamine Pathways
To see still clear please click on the figure

Dopamine takes the central place of controlling motor functions, motivation, arousal, reinforcements, executive functions and rewards at a higher level. Also, it controls functions including breastfeeding, sexual gratification and nausea at a lower level. Due to some pathological condition if dopamine is overactive and all of its above functions exceed beyond the limit it leads to a mental overactivity known as psychosis. To read further 1.click (2.here).

The above picture shows the normal pathways of dopamine in our brain. But if when a person repeatedly subjected to continuous and severe pressing situations and trauma then that person become psychotic due to the exacerbated dopamine travel.

The person goes to a psychiatrist to solve this problem. The doctor prescribes antipsychotic drugs. It is totally absurd to take drugs to solve mental problems. Because all psych drugs are neurotoxic and produce serious side effects in later periods.

All antipsychotic drugs such as haloperidol, fluphenazine, chlorpromazine, trifluoperazine, perphenazine, and thiothixene are blocking dopamine to reach its receptors and reduce its activities in the brain. Chronic use of these drugs produces serious side effects including Parkinson Disease (P.D), extrapyramidal effects like tardive dyskinesia, akathisia, bradykinesia and many other complications including anticholinergic and endocrine side effects.

Antipsychotics may not produce the required effects immediately but sedation and other side effects can occur rapidly.

Dopamine Blockade
To see clearly click on the figure

Parkinson Disease (P.D.):-

Parkinson's Disease

Continuos use of antipsychotics can cause a slow progression of P.D. due to the total loss of dopaminergic cells in the substantial nigra of the basal ganglia in the midbrain.

What are extrapyramidal side effects?

Akathesia-Motor restlessness

                                  Akathesia

Acute Dystonia-Slow and prolonged muscle spasm of tongue, neck and face.

Dystonia

Neuroleptic malignancy-Rigidity, altered mental status, cardiac arrhythmias, elevated B.P., and fatal hyperpyrexia.

                     Antidopamine Malignancy

Tardive dyskinesia-Rhythmical involuntary movements of tongue, lips or jaw. Chewing and puckering of the mouth.

                          Tardive Dyskinesia

All the above are a few of their side effects.

A recent study stated that prolonged use of antipsychotic drugs can precipitate metabolic disorders like diabetes mellitus and cardiovascular disorders.

Morally psychosis does not need bodily medication but needs mental counselling by a psychologist at its very beginning. 

But once you start medication according to a psychiatrist, then you will become a drug addict that will result in many bodily complications.

Beware of psychiatry.

BEWARE OF SLEEPING MEDICINES

SLEEPING MEDICATION-ERRORS

BLOW HOT BLOW COLD

All experts in the medical and pharmaceutical industry, including doctors, should make warnings about sleeping pills to patients and the general public. That is not only justice and virtue but also humanity.

A 2012 survey by the Food and Drug Administration (FDA) in the United States alone found that about 500,000 people die each year from sleeping pills. Suicides were not included in this survey. It only adds to the death toll of those addicted to it that I would not get any sleep if I did not take sleeping pills daily.

According to a study, regular use of sleeping pills can cause insomnia (INSOMNIA). Thus they increase the dose spontaneously without consulting a doctor. It causes more problems. 

parasomnia is one of the bad sleeping sicknesses. It also comes down to those who abuse sleeping pills. Symptoms  

1. Awakening from sleep with confusion and instability 

2. Stunning to know where we are when we wake up. Feeling alienated from our own home. Surprise.

3. Doing things without realizing it. Such as driving. Cooking.

4. Finding abnormal wounds and marks on the body 

5. Inability to sleep at night, sleeping during the day, such as a dilemma 

Somnambulance is a sleep disorder that often affects people who take sleeping pills.

The sleep that comes with a sleeping pill is a night of bad sleep. You will feel this bad sleep as soon as you wake up. The battered model would be such an asshole. A headache will come. Constipation follows. That is what will make you feel like a patient in the course of the day you will not be active. It can also cause blurred vision, dizziness, nausea, tremors, and weakness. These are all anticholinergic effects. Click here to see more clearly about this.

Sleeping pill habits can become addictive over the course of the day and make you addicted. If you are addicted like that, then your normal sleep pattern will be disturbed as if you do not have a pill, you will not get even a normal night sleep.

The pictures below illustrate how sleeping pills can affect your nerves.

Fig-1

 

As shown in Figure 1 above, the movement of a nerve is normal. The first to be shown in Level-1 from top to bottom is the Neural System of a Nerve. It contains sodium ions outside the nerve cell and potassium ions inside. Both sides contain chloride ions. Sodium ions (Na +) are generally more positively charged (POSITIVE or + -ve) ions than potassium (K +) ions. Chloride (Cl-) ions, meanwhile, are strong NEGATIVE or -ve ions. Therefore at this polarized state, the positive energy outside the nerve cell is high (+)

Inside the cell, it is either loose (+)positively charged or strong negatively charged (-) ions.

The following hormones in the central nervous system are stimulant neurotransmitters. They are,

1) Noradrenaline, 

2) dopamine, 

3) acetylcholine, 

4) glutamate and 

5)Aspartate.

When one of these hormones binds its receptor, the charged ions begin to flow through their respective gates in and out of the nerve cell. The strongly charged sodium ions flow in, with an equal effusion of potassium ions out of the nerve cells that cause a stronger ( ➕ ) positive charge inside the cell. This condition is called cell depolarization (Figure 1-Level-2).  

In this condition the nerve cell got excited. (Figure-1, stage-3)

FIG-2

Figure-2 above is the next stage of Figure-1. That is, we saw in the illustration of Figure-1 above that under normal conditions the positive energy outside the nerve cell and the negative energy inside are in equilibrium and that this state is reversed by the stimulation of nerve stimulating hormones.

In Figure-2 we can see the attacks of nerve suppressor or suppressing hormones secreted in the same central nervous system.

The inhibitory or suppressing neurotransmitter hormones secreted in the central nervous system are as follows: -

1. GABA - GAMMA-AMINOBUTYRIC ACID

2.Glycine (GLYCINE)

3.SEROTONIN or 5-HYDROXY TRYPTOPHANE

The most important of these is GABA. During normal sleep, GABA binds to its receptor in a normal state, followed by a few chloride ions enter the nerve cells and bring the nerve to a normal polarized electrical state. (Figure-2-Level-2) This is the natural sleep state.

After taking a sleeping pill, for example, alprazolam that binds to its own receptor adjacent to the GABA receptor  (Fig-2- Level-3) causes GABA to bind its receptor firmly and very intimately (Fig-2-level-3) that follows a heavy inflow of chloride ions inside the cell and causes the nerve fibre hyperpolarized, that means it attained a state of hardness to depolarize to return to its original state. (Figure-2-Level-3). That is why the sleep that comes with a sleeping pill is not a real sleep but a sense of mild to moderate unconsciousness. Death can follow if it has been given an overdose 

Eating this often will cause your nervous system to degenerate a little bit. 

Causes neurasthenia. Over the course of the day, you will find yourself feeling like a patient. 

People who should not take sleeping pills: -

1.Drinkers who usually drink alcoholic beverages such as brandy and whiskey 

2. Addicted to drugs such as cannabis, opium, cocaine, heroin 

3.Antipsychotics such as Perphenazine, Haloperidol (Haldol), Troperidol, Closaparil (Clozaril), Risperidone (Risperdal) and the drug Chlorpromazine (Largactil) should be avoided with anxiolytics

4. People who take antidepressants such as amitriptyline

5. Cholinergic antagonists 

6. Allergy medications, including cough medicines  

How to quit sleeping pill habit?

 Those who take 10 mg daily should take it as 5 mg, those who take 5 mg daily should take it as 2 mg, and those taking it daily should take 2 mg. Eat it once a week or once a month, then cut it down to once a day or twice a day and then drop the habit immediately. 

Is Melatonin Good for Sleep?

Click here to see more about it 

What are the types of sleeping pills and their individual members under each type?

Table of Sleeping Medicines

BARBITURATES

Barbiturates like Luminal (Phenobarbital), Nembutal (Pentobarbital), Amytal (Amobarbital) and Pentothal (Thiopental) are nowadays rarely used as sleeping aids because of their serious side effects. Phenobarbital is used to control seizures as an anticonvulsant.

Thiopental is used as an anaesthetic adjuvant. For more details click here.

         

 

BEWARE OF ANTICHOLINERGICS -(MUSCARINIC RECEPTOR ANTAGONISTS)

 CHOLINERGIC NERVE BLOCKADE-EFFECTS

Before going into the subject we should basically understand what is known as the cholinergic nervous system. It is far enough to describe it very briefly as the detailed description is already available in this blog under the title, Autonomic Nervous System in parts.

Fig-1

The autonomic nervous system is pharmacologically divided into two parts as follows

1.Cholinergic N.S

2.Adrenergic N.S.

Both nervous systems are working in a balanced condition. If one system is blocked medically or mechanically then the other system predominates.

But in some areas, one system predominates and in another area, another system predominates according to the necessity and situation.

The cholinergic nervous system occupies 99% of the parasympathetic nerve supply except for the one to the sweat glands which is purely sympathetic. Further details on this subject are out of our purpose.

In the figure (Fig-1) one can easily understand the supply of cholinergic nerves to various autonomous organs.

Generally in the tranquil conditions the cholinergic N.S. predominates and on contrary in the stressful situations, the adrenergic N.S predominates. Hence the cholinergic N.S is known as the tranquil N.S and the other is known as stressful N.S. For example, in normal situations, the heart is under cholinergic control, and in stressful conditions, the control is shifted to the adrenergic N.S so that the heart rate, the pulse rate, and B.P all increase.

There are many anticholinergic drugs available on the counter of the drug stores and pharmacies that are dispensed as OTC medicines without doctors' prescriptions. The main purpose of this article is to give some detailed warnings about how the patient is affected by the misuse of these drugs.

There are many anticholinergic drugs available at the pharmacy counters as cough syrups, cold and allergy medications, sleeping medicines, psychotic and antipsychotic medications, antidiarrheals and other gastrointestinal disorders medicines, ENT preparations, ophthalmic medicines, etc. etc. These are purchased by the patients either as self medications or by the doctors prescription. Anyhow if these medicines are misused and overused they may produce harmful side effects to the body.

In the above figure (Fig-1), it is clearly mapped that the cholinergic network covers almost all over our body.

The eyes are getting clear visions by the normal cholinergic nerve influence that keeps the moisture content and secretions of the eyes properly and regulate the circular and ciliary muscle contractions to accommodate the vision and the image.

Heart with its beating rate, conduction velocity, atrial contractility and the pulses followed by the blood pressure are kept normal in peaceful situations by the balanced cholinergic influence. 

Lungs and the bronchial tree are kept moisturised with their normal secretions and are properly contracted to regulate the rate of respiration, by the balanced influence of the cholinergic nerve supply.

Stomach and intestinal muscles are properly relaxed to improve the digestive system and facilitate the defecation process.

The urinary sphincter muscle is relaxed and the bladder wall is contracted by the cholinergic balanced influence to ease the bladder emptying its urine content.

The sweat glands are supplied with both the sympathetic and the parasympathetic nervous system and in both the system the postganglionic neurotransmitter is acetylcholine. The sympathetic cholinergic secretion causes localised sweating and the parasympathetic cholinergic secretion causes generalised sweating and in both cases, the body is facilitated to eliminate the excess heat.

During coital activities, the cholinergic nerve supply to the penis helps it to get sufficient erection and help both the partners to attain orgasm.

The following secretory glands secretions under the balanced influence of the cholinergic nervous system. See the figure above (Fig-1)

1.Sweat glands -They are influenced by both sympathetic and parasympathetic nervous system in which the postganglionic neuronal transmitter is acetylcholine.

2.Intestinal secretions:- They are increased by the stimulation of the cholinergic nervous system. Thus the cholinergic nervous system speeds up the process of digestion, absorption and excretion.

3.Bronchoial secretions:- These secretions are maintained and increased by the cholinergic nervous system in order to maintain the cleanliness of the respiratory pathway and to regulate the normal respiration.

4.Lacrimal (Tear) secretions:- Cholinergic nervous system help the eyes to clean itself by its secretions and to maintain the correct intra-ophthalmic pressure (IOP).

THE CHOLINERGIC BLOCKADE-ANTICHOLINERGICS:-

Fig-2

Those drugs which block the muscarinic receptors of the postganglionic cholinergic nervous system are known as anticholinergic agents (See fig-2).

There are many medications which we commonly use with or without doctors' advises including cough syrups have anticholinergic side effects that are undesired to our purpose.

Cough syrups that contain diphenhydramine hydrochloride have anticholinergic side effects and if patients who have any one of the following conditions such as benign prostatic hyperplasia, hypertension, tachyarrhythmia (heartbeat is higher and irregular), high pulse rate, dry eyes may have moderate to serious consequences.

Constipation and Gastro Oesophagal Reflex Disease are some of the common symptoms of overusing anticholinergics such as tricyclic antidepressants (amitriptyline, imipramine, and clomipramine and Thorazine), anti-Parkinson drug under the brand Cogentin(Benztropine) trihexyphenidyl (Artane),   antihistamines (diphenhydramine hydrochloride, chlorpheniramine maleate) and anti-asthmatics (Ipratropium).

There are many anticholinergic such as atropine, scopolamine, homatropine, cyclopentolate, tropicamide and pirenzepine. Atropine is the prototype to this group and is present in Atropa belladonna plant and is a belladonna alkaloid. Atropine, homatropine and scopolamine are used to relieve stomach pain, gastrointestinal spasms and stomach ulcers. If they are overused then they may precipitate anticholinergic unbearable side effects.

Atropine, homatropine, cyclopentolate and tropicamide are also used as eye drops to produce mydriasis (dilatation of the pupil) and cycloplegia (paralysis of the ciliary muscle to relieve pain due to anterior uveitis).

Antihistaminic cough syrups such as diphenhydramine hydrochloride, chlorpheniramine maleate or simply any antihistamine contain anticholinergic effects. Antihistamine fexofenadine containing medicines may have a safe therapeutic index.

Clidinium bromide and chlordiazepoxide are the familiar drugs combination under the brand names Librocol and Librax used for stomach ulcers, stomach cramp, and IBS (irritable bowel syndrome). Both the drugs in this combination have anticholinergic effects.

Urinary incontinence (uncontrolled urination due to bladder overactivity) can be treated with the anticholinergic drug known as darifenacin (Trade names Enablex, Emselex) 

Dicyclomine + Paracetamol combination under the brand names Baralgan NU, Trigan D, and Spasidex, used for IBS, intestinal and renal colics with abdominal pain is a powerful anticholinergic combination.

Flavoxate under the brand Urispas used for urinary incontinence is an anticholinergic.

Table of anticholinergics with their brand names and uses:-

A-List of Commonly Used Anticholinergics their brand names and Uses

Anticholinergic Side Effects

1. Blurred Vision 

2.Dry Mouth

3.Urinary Retention (Difficulty in passing urine)

4.Increased and irregular heartbeat.

5.Hypertention

6.Hellucinations, delusions, tinnitus, and dementia

7.Constipation, bowel obstruction

8.Decreased sweating and hyperthermia.

In general, those who are regularly taking medicines such as antipsychotic drugs, antihistaminic drugs to treat allergy, cough, asthma and urticaria must be careful to watch the symptoms of the side effects.

Whenever any drug if you have to take chronically, please get in touch with your doctor intermittently.