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Anticholinergic

 

 
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Anticholinergic
 
 
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An anticholinergic agent is a substance that blocks the neurotransmitter
Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
 acetylcholine
Acetylcholine

The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including homo sapiens....
 in the central
Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
 and the peripheral nervous system
Peripheral nervous system

The peripheral nervous system resides or extends outside the central nervous system , which consists of the brain and spinal cord. The main function of the PNS is to connect the CNS to the limbs and organs....
. An example of an anticholinergic is dicyclomine
Dicyclomine

Dicyclomine is an anticholinergic that blocks muscarinic acetylcholine receptor. Dicyclomine is known as dicycloverine hydrochloride in the UK....
. Frequently, they reduce the effects mediated by acetylcholine on acetylcholine receptors
Transmembrane receptor

Transmembrane receptors are integral membrane proteins, which reside and operate typically within a cell's plasma membrane, but also in the biological membrane of some subcellular compartments and organelles....
 in neuron
Neuron

Neurons are responsive cell in the nervous system that process and transmit information by electrochemical Signal . They are the core components of the brain, the vertebrate spinal cord, the invertebrate ventral nerve cord, and the peripheral nerves....
s through competitive inhibition. Therefore, their effects are reversible.

Anticholinergics are classified according to the receptors that are affected:

cholinergic drugs are used in treating such conditions as the following:

• Gastrointestinal disorders (eg, gastritis
Gastritis

Gastritis is an inflammation of the lining of the stomach, and has many possible causes. The main acute causes are excessive alcohol consumption or prolonged use of nonsteroidal anti-inflammatory drugs such as aspirin or ibuprofen....
, pylorospasm, diverticulitis
Diverticulitis

Diverticulitis is a common digestive disease particularly found in the colon . Diverticulitis develops from diverticulosis, which involves the formation of pouches on the outside of the colon ....
, ulcerative colitis
Ulcerative colitis

Ulcerative colitis is a form of inflammatory bowel disease . Ulcerative colitis is a form of colitis, a disease of the intestine, specifically the large intestine or colon , that includes characteristic Peptic ulcer, or open sores, in the colon....
)

• Genitourinary disorders (eg, cystitis
Cystitis

Cystitis is inflammation of the urinary bladder. The condition more often affects women, but can affect either sex and all age groups....
, urethritis
Urethritis

Urethritis is inflammation of the urethra. The main symptom is dysuria, which is painful or difficult urination....
, prostatitis
Prostatitis

Prostatitis is an inflammation of the prostate gland, in men. A prostatitis diagnosis is assigned at 8% of all urologist and 1% of all primary care physician visits in the United States....
)

• Respiratory disorders (eg, asthma
Asthma

Asthma is a common chronic obstructive pulmonary disease, in which the Lung constrict, become inflammation, and are lined with excessive amounts of thickened mucus, often in response to one or more triggers....
, chronic bronchitis
Chronic bronchitis

Chronic bronchitis is a chronic inflammation of the bronchus in the lungs. It is generally considered one of the two forms of chronic obstructive pulmonary disease ....
)

• Parkinson’s disease and Parkinson-like adverse medication effects

When a significant amount of an anticholinergic is taken into the body, a toxic reaction
Toxidrome

In medicine, a toxidrome is a syndrome caused by a dangerous level of toxins in the body. It is often the consequence of a drug overdose. Common symptoms include dizziness, disorientation, nausea, vomiting, and oscillopsia....
 known as acute anticholinergic syndrome may result.






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Encyclopedia


An anticholinergic agent is a substance that blocks the neurotransmitter
Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
 acetylcholine
Acetylcholine

The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including homo sapiens....
 in the central
Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
 and the peripheral nervous system
Peripheral nervous system

The peripheral nervous system resides or extends outside the central nervous system , which consists of the brain and spinal cord. The main function of the PNS is to connect the CNS to the limbs and organs....
. An example of an anticholinergic is dicyclomine
Dicyclomine

Dicyclomine is an anticholinergic that blocks muscarinic acetylcholine receptor. Dicyclomine is known as dicycloverine hydrochloride in the UK....
. Frequently, they reduce the effects mediated by acetylcholine on acetylcholine receptors
Transmembrane receptor

Transmembrane receptors are integral membrane proteins, which reside and operate typically within a cell's plasma membrane, but also in the biological membrane of some subcellular compartments and organelles....
 in neuron
Neuron

Neurons are responsive cell in the nervous system that process and transmit information by electrochemical Signal . They are the core components of the brain, the vertebrate spinal cord, the invertebrate ventral nerve cord, and the peripheral nerves....
s through competitive inhibition. Therefore, their effects are reversible.

Anticholinergics are classified according to the receptors that are affected:
  • Antimuscarinic agents operate on the muscarinic acetylcholine receptor
    Muscarinic acetylcholine receptor

    Muscarinic receptors, or mAChRs, are G protein-coupled receptor acetylcholine receptors found in the plasma membranes of certain neurons and other Cell s....
    s. The majority of anticholinergic drugs are antimuscarinics.
  • Antinicotinic agents operate on the nicotinic acetylcholine receptor
    Nicotinic acetylcholine receptor

    Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons....
    s.


Effects

Anticholinergic drugs are used in treating such conditions as the following:

• Gastrointestinal disorders (eg, gastritis
Gastritis

Gastritis is an inflammation of the lining of the stomach, and has many possible causes. The main acute causes are excessive alcohol consumption or prolonged use of nonsteroidal anti-inflammatory drugs such as aspirin or ibuprofen....
, pylorospasm, diverticulitis
Diverticulitis

Diverticulitis is a common digestive disease particularly found in the colon . Diverticulitis develops from diverticulosis, which involves the formation of pouches on the outside of the colon ....
, ulcerative colitis
Ulcerative colitis

Ulcerative colitis is a form of inflammatory bowel disease . Ulcerative colitis is a form of colitis, a disease of the intestine, specifically the large intestine or colon , that includes characteristic Peptic ulcer, or open sores, in the colon....
)

• Genitourinary disorders (eg, cystitis
Cystitis

Cystitis is inflammation of the urinary bladder. The condition more often affects women, but can affect either sex and all age groups....
, urethritis
Urethritis

Urethritis is inflammation of the urethra. The main symptom is dysuria, which is painful or difficult urination....
, prostatitis
Prostatitis

Prostatitis is an inflammation of the prostate gland, in men. A prostatitis diagnosis is assigned at 8% of all urologist and 1% of all primary care physician visits in the United States....
)

• Respiratory disorders (eg, asthma
Asthma

Asthma is a common chronic obstructive pulmonary disease, in which the Lung constrict, become inflammation, and are lined with excessive amounts of thickened mucus, often in response to one or more triggers....
, chronic bronchitis
Chronic bronchitis

Chronic bronchitis is a chronic inflammation of the bronchus in the lungs. It is generally considered one of the two forms of chronic obstructive pulmonary disease ....
)

• Parkinson’s disease and Parkinson-like adverse medication effects

When a significant amount of an anticholinergic is taken into the body, a toxic reaction
Toxidrome

In medicine, a toxidrome is a syndrome caused by a dangerous level of toxins in the body. It is often the consequence of a drug overdose. Common symptoms include dizziness, disorientation, nausea, vomiting, and oscillopsia....
 known as acute anticholinergic syndrome may result. This may happen accidentally or intentionally as a consequence of recreational drug use
Recreational drug use

Recreational drug use is the use of psychoactive drugs for recreational purposes rather than for employment, Medicine or Spirituality purposes, although the distinction is not always clear ....
. Anticholinergic drugs are usually considered the least enjoyable by experienced recreational drug users, possibly due to the lack of euphoria caused by them. (For some of the recreational effects, see the article on deliriant
Deliriant

The deliriants are a special class of acetylcholine receptor-inhibitor dissociatives. The name comes from their primary effect of inducing a medical state of frank delirium, characterized by stupor, utter confusion, confabulation, and regression to "phantom" behaviors such as disrobing and plucking ....
s.) Because most users do not enjoy the experience, they do not use it again, or do so very rarely. The risk of addiction is low in the anticholinergic class. The effects are usually more pronounced in the elderly, due to natural reduction of acetylcholine production associated with age.

Possible effects of anticholinergics include:
  • Ataxia
    Ataxia

    Ataxia is a neurology sign and symptom consisting of gross lack of coordination of muscle movements. Ataxia is a non-specific clinical manifestation implying dysfunction of parts of the nervous system that coordinate movement, such as the cerebellum....
    ; loss of coordination
  • Decreased mucus production in the nose and throat
    Throat

    In anatomy, the throat is the anterior part of the neck, in front of the vertebrae. It consists of the pharynx and larynx. An important feature of the throat is the epiglottis, a flap which separates the esophagus from the vertebrate trachea and prevents inhalation of food or drink....
    ; consequent dry, sore throat
  • Xerostomia
    Xerostomia

    Xerostomia is the medical term for a dry mouth due to a lack of saliva. Xerostomia is sometimes colloquially called pasties, cottonmouth, or doughmouth....
     or dry mouth with possible acceleration of caries
  • Cessation of perspiration; consequent decreased epidermal thermal dissipation leading to warm, blotchy, or red skin
  • Increased body temperature
  • Pupil dilation (mydriasis
    Mydriasis

    Mydriasis is an excessive dilation of the pupil due to disease, Physical trauma, or the use of drugs. Normally, the pupil dilates in the dark and constriction in the light to improve vividity at night and to protect the retina from sunlight damage during the day....
    ); consequent sensitivity to bright light (photophobia
    Photophobia

    Photophobia is a symptom of excessive sensitivity to light and the aversion to sunlight or well-lit places. In medical terms it is not fear, but an experience of discomfort or pain to the eyes due to light exposure....
    )
  • Loss of accommodation (loss of focusing ability, blurred vision — cycloplegia
    Cycloplegia

    Cycloplegia is paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation . ...
    )
  • Double vision (diplopia
    Diplopia

    Diplopia, commonly known as double vision, is the simultaneous perception of two images of a single object. These images may be displaced horizontally, vertically, or diagonally in relation to each other....
    )
  • Increased heart rate (tachycardia
    Tachycardia

    The word tachycardia comes from the Greek words tachys and kardia .Tachycardia typically refers to a heartrate that exceeds the range of the normal resting heartrate, based upon age:...
    )
  • Easily startled
  • Urinary retention
    Urinary retention

    Urinary retention also known as ischuria is a lack of ability to urinate. It is a common complication of Benign prostatic hyperplasia , although anticholinergics may also play a role, and requires a catheter or Prostatic stent....
  • Diminished bowel movement, sometimes ileus
    Ileus

    Ileus is a disruption of the normal propulsive gastrointestinal tract motor activity from non-mechanical mechanisms. Motility disorders that result from structural abnormalities are termed mechanical bowel obstruction....
  • Increased intraocular pressure
    Intraocular pressure

    Intraocular pressure is the fluid pressure inside the eye....
    , dangerous for people with narrow-angle glaucoma
    Glaucoma

    Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
  • Shaking


Possible effects in the central nervous system
Central nervous system

The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms....
 resemble those associated with delirium
Delirium

Delirium is an acute and relatively sudden decline in attention-focus, perception, and cognition. In medical usage it is not synonymous with drowsiness, and may occur without it....
, and may include:
  • Confusion
  • Disorientation
  • Agitation
  • Euphoria
    Euphoria

    Euphoria or euphoric may refer to:* Euphoria , an emotional and mental state Defined as a sense of great elation and wellbeing* 4-Methyl-aminorex , a stimulant drug with effects comparable to methamphetamine...
     or dysphoria
    Dysphoria

    Dysphoria is generally characterized as an unpleasant or uncomfortable mood, such as sadness , anxiety, irritability, or restlessness. Etymologically, it is the opposite of euphoria ....
  • Respiratory depression
  • Memory problems
  • Inability to concentrate
  • Wandering thoughts; inability to sustain a train of thought
    Train of thought

    The train of thought, stream of thought, or chain of thought refers to the interconnection in the sequence of ideas expressed during a connected discourse or thought, as well as to the sequence itself, especially in discussion how this sequence leads from one idea to another....
  • Incoherent speech
  • Wakeful myoclonic jerking
  • Unusual sensitivity to sudden sounds
  • Illogical thinking
  • Photophobia
  • Visual disturbances
    • Periodic flashes of light
    • Periodic changes in visual field
    • Visual snow
      Visual snow

      Visual snow is a transitory or persisting visual symptom where people see noise or television-like Noise in parts or the whole of their visual fields, especially against dark backgrounds....
    • Restricted or "tunnel vision"
  • Visual, auditory, or other sensory hallucination
    Hallucination

    A hallucination, in the broadest sense, is a perception in the absence of a stimulus . In a stricter sense, hallucinations are defined as perceptions in a conscious and awake state in the absence of external stimuli which have qualities of real perception, in that they are vivid, substantial, and located in external objective space....
    s
    • Warping or waving of surfaces and edges
    • Textured surfaces
    • "Dancing" lines; "spiders", insects
    • Lifelike objects indistinguishable from reality
    • Hallucinated presence of people not actually there
  • Rarely: seizures, coma and death


Acute anticholinergic syndrome is completely reversible and subsides once all of the toxin has been excreted. Ordinarily, no specific treatment is indicated. However, in extreme cases, especially those that involves severe distortions of mental state, a reversible cholinergic
Cholinergic

A receptor is cholinergic if it uses acetylcholine as its neurotransmitter.Cholinergic means related to the neurotransmitter acetylcholine, and is typically used in a neurological perspective....
 agent such as physostigmine
Physostigmine

Physostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor alkaloid of the Calabar bean.The chemical was synthesized for the first time in 1935 by the chemists Percy Lavon Julian and Josef Pikl....
 may be used.

Plant sources

The most common plants containing anticholinergic alkaloids are:
  • Atropa belladonna (Deadly Nightshade)
  • Brugmansia
    Brugmansia

    Brugmansia is a genus of six species of flowering plants in the family Solanaceae, native to subtropical regions of South America, along the Andes from Colombia to northern Chile, and also in southeastern Brazil....
     species (Brugmansia)
  • Datura
    Datura

    Datura is a genus of nine species of Vespertine flowering plants belonging to the family Solanaceae. Their exact natural distribution is uncertain, due to extensive cultivation and naturalisation throughout the temperate and tropical regions of the globe, but is most likely restricted to the Americas, from the United States south throug...
     species (Datura)
  • Hyoscamus niger
    Henbane

    Henbane , also known as stinking nightshade, is a plant of the family Solanaceae that originated in Eurasia, though it is now globally distributed....
     (Henbane)
  • Mandragora officinarum
    Mandrake (plant)

    Mandrake is the common name for members of the plant genus Mandragora belonging to the nightshades family . Because mandrake contains deliriant hallucinogenic tropane alkaloids such as hyoscyamine and the roots sometimes contain bifurcations causing them to resemble human figures, their roots have long been used in magic rituals, t...
     (Mandrake)


Use as a deterrent

Certain preparations of some drugs, such as Hydrocodone
Hydrocodone

Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from two of the naturally-occurring opiates codeine and thebaine....
, are mixed with an anticholinergic agent to deter intentional overdose.