Scribd Logo
Upload

Welcome to Scribd!

  • 31 views

    Hypnosedative Drugs 17.10.2023

    Uploaded by

    Nuhu Siba
    1. Hypnosedative drugs like benzodiazepines and barbiturates act through the GABA-A receptor to cause sedation and hypnosis. They work by facilitating the entry of chloride ions into neurons, which hyperpolarizes the cells and leads to inhibition. 2. Benzodiazepines are commonly used as anxiolytics, hypnotics, and for treating conditions like epilepsy and panic attacks. Short-acting benzodiazepines are more addictive and cause more side effects than long-acting ones. 3. While benzodiazepines are generally safer than barbiturates, both classes of drugs can cause tolerance, dependence, and

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd

    Hypnosedative Drugs 17.10.2023

    Uploaded by

    Nuhu Siba
    31 views49 pages
    1. Hypnosedative drugs like benzodiazepines and barbiturates act through the GABA-A receptor to cause sedation and hypnosis. They work by facilitating the entry of chloride ions into neurons, which hyperpolarizes the cells and leads to inhibition. 2. Benzodiazepines are commonly used as anxiolytics, hypnotics, and for treating conditions like epilepsy and panic attacks. Short-acting benzodiazepines are more addictive and cause more side effects than long-acting ones. 3. While benzodiazepines are generally safer than barbiturates, both classes of drugs can cause tolerance, dependence, and

    Copyright

    © © All Rights Reserved

    Available Formats

    PPTX, PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    1. Hypnosedative drugs like benzodiazepines and barbiturates act through the GABA-A receptor to cause sedation and hypnosis. They work by facilitating the entry of chloride ions into neurons, which hyperpolarizes the cells and leads to inhibition. 2. Benzodiazepines are commonly used as anxiolytics, hypnotics, and for treating conditions like epilepsy and panic attacks. Short-acting benzodiazepines are more addictive and cause more side effects than long-acting ones. 3. While benzodiazepines are generally safer than barbiturates, both classes of drugs can cause tolerance, dependence, and

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    31 views49 pages

    Hypnosedative Drugs 17.10.2023

    Uploaded by

    Nuhu Siba
    1. Hypnosedative drugs like benzodiazepines and barbiturates act through the GABA-A receptor to cause sedation and hypnosis. They work by facilitating the entry of chloride ions into neurons, which hyperpolarizes the cells and leads to inhibition. 2. Benzodiazepines are commonly used as anxiolytics, hypnotics, and for treating conditions like epilepsy and panic attacks. Short-acting benzodiazepines are more addictive and cause more side effects than long-acting ones. 3. While benzodiazepines are generally safer than barbiturates, both classes of drugs can cause tolerance, dependence, and

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 49

    Hypnosedative Drugs

    Dr. Maryam Mohammadzadeh


    Hypnosedative Drugs
    • These drugs are drugs that make you sleep (as insomnia medications)
    and at the same time drowsy. In other words, these group of drugs
    cause sedation and hypnosis and roughly we call these drugs
    Benzodiazepines and Barbiturates.
    amine-like neurotransmitters
    • neurotransmitters with amino acid structure (inhibitors)
    • GABA (Gamma Amino Butyric acid)
    • Glycine
    GABA (Gamma Amino Butyric acid)
    • Gamma-aminobutyric acid (GABA): This naturally occurring amino
    acid acts as the body's main inhibitory chemical messenger. GABA
    contributes to vision, motor control, and plays a role in the regulation of
    anxiety. Benzodiazepines, which are used to help treat anxiety, function by
    increasing the efficiency of GABA neurotransmitters, which can increase
    feelings of relaxation and calm.
    • Synthesized from glutamate (glutamic acid) by gulutamic acid decarboxylase.
    The effect of GABA in the synaptic cleft ends with reuptake.

    It is broken down by the GABA transaminase into succinic semialdehyde.


    GABA receptors
    • GABA is the most important inhibitor of the central nervous system.

    • It has three receptors, GABA A, GABA B and GABA C.

    • GABAA and GABAc are ion channel receptors that introduce chlorine
    ion into the cell,

    • GABAB is the receptor that inhibits adenylate cyclase via Gi.


    GABA A receptor

    • As a result of Cl- channel opening, it increases the size of the intracellular


    negative charge, causing hyperplarization and leads to inhibition.

    • GABA A receptor agonist is muscimol, and antagonist of GABA is Bicukulin.

    • Benzodiazepines and barbiturates are GABA A agonist drugs.

    • Picrotoxin and pentylenetetrazole are antagonists of the Cl-channel through


    the GABA A receptor, creating analeptic and convulsive effects
    • Picrotoxin and pentylenetetrazole are antagonists of the Cl-channel
    through the GABA A receptor, creating analeptic and convulsive
    effects. These toxins are used to induce experimental epilepsy in
    animals.
    GABA B RECEPTOR
    • The GABA B receptor is coupled with Gi.
    • They are not affected by benzodiazepines and barbiturates.
    • GABA B agonist drug Baclofen antagonist drug is phacolofen and
    saclofen
    GABA C
    • It is the ion channel receptor, selective to cl- ions. It is found in the
    retina, medulla spinalis, superior culliculus and pituitary.
    Glycine
    • The most important inhibitor in the medulla spinalis and brain stem is
    glycine.

    • It is an ion channel receptor with GABA-like chlorine channel activity.

    • Strychnine inhibits glycine ion channels thereby preventing Cl entry


    into the neuron and causing convulsions.
    • If there is strychnine poisoning, the medication we will give are anti-
    epileptic drugs (benzodiazepines, barbiturates).
    Mechanism Of Action Of Hypnosedative Drugs

    • These drugs are drugs that act through GABA A. They are drugs that cause
    CL-entry into the neuron. Inhibition increases when CL- enters the cell, and
    these drugs act as anti-convulsant.
    • Then CL- enters the neuron cell, inhibition increases, and these drugs act as
    anticonvulsant.
    • When CL- enters the cell, the striated muscles relax because a negative ion has
    entered the cell.
    • These drugs are addictive and can be abused, their effects develop tolerance.
    • These drugs eliminate anxiety.
    • Benzodiazepines are lipophilic drugs. Because the GABAA
    receptor is in the brain, they easily pass into the brain

    • Benzodiazepines make hypnosedative effects through allosteric


    interactions on GABA A receptor.
    • Allostric interaction
    • There is a benzodiazepine receptor next to the GABA A
    receptor. Benzodiazepine binds to the BZ receptor and
    stimulates it, the channel opens to CL- enters the content
    through GABAA,
    • who introduced Cl- into the cell?
    • GABAA itself contains the cl- ion, Benzodiazepines indirectly
    activate GABA A,
    It means, benzodiazepine increases the activity of GABA receptors and
    the opening frequency of chlorine ion channels by binding to its
    receptors (BZ receptor).
    GABA must be present in the environment for benzodiazepines to work.
    • If the hypnosedative drug is short-acting, or short-acting benzodiazepines
    and barbiturates are more addictive, more tolerant, more sleep
    disturbances, more psychotic side effects.

    • Long-acting hypnosedative drugs ( Benz\Barb) cause hangover.

    • short acting benzodiazepines Midazolam and Triazolam


    • short-acting barbiturates are methohexital and thiopental.
    The main differences of benzodiazepines and
    barbiturates:

    • Not a scientific explanation, but Barbiturates in general are bad, benzo


    diazepines are good

    • Why?????
    • Because;
    • Barbiturates make enzyme induction, that is, they increase the destruction of
    many drugs.

    • they cause hyperalgesia, that is, the pain gets worse

    • more addiction and tolerance develop

    • They make more sleep disturbances

    • therapeutic ranges are narrower.

    • anticonvulsant effects are greater


    • BUT ; Benzodiazepines have GABA dependent effects
    • do not induce enzyme

    • Less addiction and tolerance develop

    • Make less sleep disturbances

    • Therapeutic ranges are wider.

    • Less anticonvulsant effects

    • Respiratory and cardiovascular effects are less.


    Benzodiazepines
    • Short acting drugs
    • Triazolam
    • Midazolam • Anxiolytic drugs
    • Alprazolam
    • long acting • Clonazepam
    • Diazepam • Diazepam
    • Flurazepam
    • Hypnotic
    • doctor uses a short-acting drug for sleeping • Triazolam
    in anesthesia, so he / she gives hypnotic • Midazolam
    drugs and the patient sleeps immediately.
    The Effects of Benzodiazepines
    • Benzodiazepines are the number one drugs for anxiety (have anxiolytic effects).
    • They create an antiepileptic effect (Cl– ions enter the cell )
    • It is used in the treatment of panic attacks and agoraphobia other than anxiety.
    • Alprazolam (xanax) is especially used in the treatment of panic attacks and
    agoraphobia.(is a type of anxiety disorder in which you fear and avoid places or
    situations that might cause you to panic and make you feel trapped, helpless or
    embarrassed. You fear an actual or anticipated situation, such as using public
    transportation, being in open or enclosed spaces, standing in line, or being in a crowd)
    • They cause muscle relaxation (Cl– ions enter the cell )
    The Effects of Benzodiazepines

    • Benzodiazepines cause sleep, but this sleep is not quality sleep. The
    patient sleeps but wakes up as if he has been kicked.
    clinical use of benzodiazepines
    • Benzodiazepine has a preanesthetic effect
    • Midazolam

    • Benzodiazepines are not antidepressants, but the antidepressant drug is


    Alprazolam.

    • panic attack treatment


    • Alprazolam
    • Antiepileptic effect
    • Diazepam, Lorazepam and midazolam are primarily preferred drugs in the
    treatment of status epilepticus.
    • In status epilepticus, the first choice is Diazepam, the second preference is
    phenobarbital.

    • Absence seizure treatment and myoclonic seizure


    • Clonazepam
    • Are benzodiazepines suitable for epilepsy prophylaxis?

    • They are not suitable for long-term treatment, the patient sleeps every
    minute,and cuases withdrawal attacks and addiction
    • Mania
    • (Mania is an abnormally elated mental state, typically characterized by feelings of euphoria, la
    ck of inhibitions, racing thoughts, diminished need for sleep, talkativeness, risk taking, and irri
    tability. In extreme cases, mania an induce hallucination and other psychotic
    • Clonazepam
    • all Benzodiazepines cause muscle relaxation
    • Diazepam
    • Clonazepam

    • In the treatment of agoraphobia


    • Alprazolam

    • sleeping pill of course short acting medicine


    • Triazolam
    • In alcohol withdrawal
    • diazepam
    • Chlordiazepoxide

    • Sleeping pill
    • Quazepam
    • Estazolam
    • Triazolam
    • Temazepam
    Benzodiazepines

    • The longest acting Benzodiazepine


    • Flurazepam

    • The shortest acting Benzodiazepine

    • Midazolam and Triazolam

    • Duration of action are listed from highest to lowest;


    • Lorazepam
    • Clorazepat
    • Diazepam
    Many Benzodiazepines are active, both
    themselves and their metabolites.
    Psychological side effects of
    Benzodiazepines;

    • Hallucination

    • Euphoria

    • If a drug is addictive, it necessarily causes hallucinations and euphoria

    • suicide attempt

    • addiction abuse
    Psychological side effects of Benzodiazepines;

    • All benzodiazepines have clinical use, Benzodiazepine Flunitrazepam without clinical


    use because (makes amnesia)

    • Psychological reactions,Delirium
    (Triazolam)

    • In addicted mother, causes the deprivation in infants crisis

    • nightmares
    • Flurazepam
    Benzodiazepines that do not form active metabolites

    • It means ; Benzodiazepines, which are active themselves and whose


    metabolites are not activated in the body;

    • Lorazepam
    • Oxazepam
    • Estazolam

    • Clonazepate is Benzodiazepine that is inactive when taken.itself is


    inactive and becomes active in the body. İt means; it is a prodrug
    Zolpidem, Zopiclone, Zaleplon ,Indiplon

    • Although they are not benzodiazepines, BZ1 receptor agonists are drugs. that is,
    drugs that bind to GABA A.
    • They use it to treat insomnia and anxiety
    • They are the drugs that change physiological sleep the least. they no longer have an
    hangover effect.

    • Flumazenil is a competetive antagonist of Benzodiazepines in Benzodiazepine


    poisoning.
    Barbiturates
    • Let's say the open time is 10 seconds, normally 5 Cl ions enter the
    content through this channel.When we give barbiturate,
    • 10 seconds is extended to 20 seconds and this time 10 Cl- ions enter
    the channel.
    • But when we give Benzodiazepines, 10 seconds does not change,
    remains constant.this time more Cl- enters the cell.so the frequency is
    increasing.
    • Barbiturates increase the binding of GABA to the GABA A receptor.

    • Both Benzodiazepines and Baebiturates bind to GABA A receptors.

    • shortest acting Barbiturates


    • Methohexital
    • Thiopental

    • longest acting Barbiturates


    • Phenobarbital
    Effects of barbiturates
    • Barbiturates are anticonvulsants because they cause Cl- entry into the
    content,

    • Short-acting Barbiturates are used in anesthesia such as Thiopental


    and metohegzital. Their effect ends with redustribution. Because
    Barbiturates are drugs that reduce intracranial pressure.

    • Barbiturates cause euphoria and cause addiction.


    • Barbiturates make enzyme induction. therefore they are not given for
    some diseases such as porphyria.

    • Barbiturates make enzyme induction. Therefore, they are not given in


    some diseases such as porphyria. In this disease,already the activity of
    ALA synthase enzyme is increased, when we give this drug to a
    person with porphyria, a bad picture may ocur.

    • causes hyperalgesia
    Clinical uses of barbiturates
    • Barbiturates are an alternative to Benzodiazepines.

    • febrile convulsion. (first choice is Diazepam, our substitute is Phenobarbital)

    • They are given in hyperbiliruminemia.

    • Short effects such as Thiopental and methohexital are given in anesthesia.

    • Phenobarbitals are the second preferred drugs after Benzodiazepines (Diazepam) in cases
    such as emergency treatment of convulsions, tetanus, status epilepticus, eclampsia, citricine
    poisoning..
    • In barbiturate poisoning, the drug we will give is Sodium bicarbonate
    because it is acid.
    alcohol

    • Alcohol is not a drug, but rather a socially used arbitrary substance.

    • When we say alcohol, the first thing that comes to mind is ethyl
    alcohol.
    • Side effects of alcohol, drunkenness,
    tachycardia, sweating, flushing, nausea
    and vomiting are related to the
    accumulated acetaldehyde.

    • If we inhibit aldehyde dehydrogenase,


    acet aldehyde accumulates, and alcohol-
    related unpleasant side effects occur.
    Inhibiting aldehyde dehydrogenase is
    used to quit alcohol. Because the person
    takes alcohol and instead of enjoying it,
    nausea becomes vomiting and therefore
    disgust alcohol.
    • The drug given to ethyl alcohol addicts is called Disulfiram.
    • Chlorpropamide, Tolbutamide, Metronidazole, Cefotetan and Trimethoprim
    produce Disulfiram-like effect when taken together with alcohol.
    Methyl Alcohol Poisoning
    • The substance responsible for the toxic effect is the accumulated Formaldehyde.

    • formaldehyde does not cause side effects, like ethyl alcohol, it has a more serious
    effect.
    • Damage due to the retina causes ırreversible blindness.

    • Treatment;

    • The substance to be given in methyl alcohol poisoning,is ethyl alcohol(10%) (IV),


    Because alcohol dehydrogenase enzymes bind to ethyl alcohol with higher affinity, the
    reaction continues in the ethyl alcohol pathway and acetaldehyde is formed instead of
    formaldehyde. so less toxic substances are formed.
    • .
    • Fomepizole inhibits the formation of Formaldehyde by inhibiting alcohol
    dehydrogenase.

    • Whether we give ethyl alcohol or Fomepizol ultimately there is methyl alcohol in


    the body, it is necessary to dialysis to destroy this substance, because then the
    enzymes become active and the methyl alcohol turns into formaldehyde again, and a
    bad situation occurs.
    • To benefit from dialysis, most of the drug will be free and the place where the
    drug is remove must be in the kidney.

    • Methyl alcohol is low bound to proteins in the body.

    You might also like