WEEK 7 Flashcards by maui lang 2 .

A very important structure of the CNS is its protective mechanisms that not all chemicals can pass through it, this affects the pharmacodynamics of drugs because some of them cannot penetrate the CNS.

Brain & Spinal Cord

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Electrical transmission of
impulses happen by_______ and____________ make use of neurotransmitters to achieve its functions

action potential

chemical processes

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Synapses made by the peripheral nervous system conduct impulses that are chemical in nature.

Autonomic Nervous System & Somatic Nervous System

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conduct impulses by Action Potential

Neurons

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movement of sodium into the cells causing

depolarization

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potassium out of the cells to cause

repolarization

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feeling of tension, nervousness, apprehension or fear that usually involves unpleasant reactions to a stimulus, whether actual or unknown

Anxiety

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Anxiety is classified as

mild, moderate, severe and panic

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severe sedation.

Hypnosis

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loss of awareness and reaction to environmental stimuli

Sedation

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GABA

Gamma
Amino Butyric Acid

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an inhibitory neurotransmitter to decrease impulses in the synapses of the brain, therefore decreasing conduction of rapid impulses causing symptoms of anxiety.

Gamma
Amino Butyric Acid

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drug action is to enhance GABA

effect. This is used to be the drug of choice to manage anxiety but its depressant effect may cause severe respiratory depression that this is not primarily used for anxiety today

Barbiturates

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drug action is to enhance GABA effect to cause inhibition of impulse transmission.

Benzodiazepines

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For overdose of Benzodiazepine

Flumazenil

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affective disorder is recognized by its clinical manifestations such as sleep disturbances, they have little energy, inability to perform daily activity. They may describe overwhelming feelings of sadness, despair, hopelessness and disorganization.

Depression

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This theory explains that depression occurs due to decreasing neurotransmitters, norepinephrine, serotonin and dopamine.

Biogenic Amine Theory.

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inhibit
presynaptic reuptake of neurotransmitter, norepinephrine and serotonin, which leads to accumulation of these neurotransmitters in the synaptic cleft and increased stimulation of postsynaptic receptors.

Tricyclic Antidepressants (TCA)

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CASH

C – Cardiovascular effects
A – Anticholinergic effects
S – Sedation
H – Hypotension or Hypertension

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These drugs inactivate the enzyme MAO
to increase the neurotransmitters in the
synapses.

MonoAmine Oxidase Inhibitors

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rich food which normally broken down by MAO enzymes in the GIT maybe absorbed in high concentration in the presence of MAOI and may cause hypertensive crises.

Tyramine

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these drugs specifically block the reuptake of serotonin with little or no effect on Norepinephrine. SSRIs do not have the many adverse effects of TCAs and MAOIs

Selective Serotonin Reuptake Inhibitors (SSRI)

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Have_______ or another________ for hypertensive crisis

phentolamine

adrenergic blocker

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is the most common type of psychotic disorder. This prevents an individual from functioning in society. Some clinical manifestations include, hallucinations, delusions, paranoia, speech abnormalities and affective problems.

Schizophrenia

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is associated with Bipolar illness. is characterized by periods of extreme overactivity and excitement

Mania

Drugs for mental disorders

Psychotherapeutic drugs

Drugs for Schizophrenia

Antipsychotic Drugs

drugs for Mania

Anti Manic Drugs.

block Dopamine receptors in the limbic system, in the reticular activating system and the brain. This group of antipsychotic may block all dopamine receptors including those not associated with psychoses

Typical Antipsychotic drugs

block Dopamine and Serotonin receptors. This group will lock only the receptors of Dopamine and Serotonin which are responsible for occurrence of psychosis

Atypical Antipsychotic drugs

ASHE

■ A – Anti cholinergic effect ■ S – Sedation ■ H – Hypotension ■ E – Extra pyramidal Symptoms

alters sodium transport in the nerve and muscle, inhibits the release of norepinephrine and dopamine slightly and decreases intraneuronal content of second messengers.

Lithium

CNS problems including lethargy, slurred speech, muscle weakness, fine tremor; polyuria, beginning gastric toxicity

Serum level less than 1.5 mmol/L

Intensification of the above plus ECG changes

Serum level 1.5 – 2 mmol/L

LProgression of CNS symptoms to ataxia, hyperreflexia and seizure, hypotension

Serum levels of 2.0 – 2.5 mmol/L

complex multi organ toxicity and death

Serum levels more than 2.5 mmol/L

Toxicity associated with serum level of Lithium. ( Therapeutic level

0.6 – 1.2

is a collection of different syndromes characterized by abnormal and excessive impulse transmission in the brain

Seizure

disorder has no known cause; this is often called Epilepsy.

Primary seizure

may be caused by Cerebrovascular accident, Infections, Brain Tumor, Traumatic Brain Injury, Fever and a lot more conditions that may alter impulse transmission in the brain.

Secondary Seizure

is seizure manifesting motor symptoms like tonic clonic seizure.

Convulsion

begins in one area of the brain and rapidly spreads to both hemispheres of the brain.

Generalized seizure

Tonic – Clonic Seizure formerly known as

Grand Mal Seizure

involve one area of the brain and do not spread throughout the entire organ.

Partial seizures or focal seizures

inhibit sodium influx or depolarization along the nerve fiber.

Hydantoins

is not used for long term treatment of seizures.

Diazepam

is good for treatment of Petit Mal Seizure and Myoclonic Seizure

Clonazepam

enhanced effect of GABA, an inhibitory neurotransmitter.

Succinimides

reduces electrical activity by suppressing calcium influx and enhancing GABA effects the drug of choice for treating myoclonic seizure

Valproate or Valproic Acid

is a degenerative disorder of the central nervous system. There is no known cause. This is common among elderly 60 years old and above. The disease is characterized by degeneration of the substantia nigra in the midbrain. A dopamine secreting neurons in the brain. Therefore there is a tremendous decrease of dopamine in the brain especially affecting the basal ganglia. The basal ganglia is responsible for coordinating fine motor movement of the body.

Parkinson’s Disease

In Parkinson’s disease an imbalance of neurotransmitters, ______________and ______________results to clinical manifestations causing incoordination for unconscious muscle movements including those that control position, posture and movement

decreased dopamine increased acetylcholine

increase the effect of Dopamine at the receptor sites by increasing the levels of dopamine in the substantia nigra or directly stimulating the receptors

Dopaminergic drug

a precursor of Dopamine. Once it enters the BBB, it becomes dopamine and will replace the loss of dopamine

Levodopa

levodopa can be destroyed by and enzyme called

dopa decarboxylase

This drug cannot increase the level of dopamine in the brain but it inhibits the enzyme, dopa decarboxylase, therefore allowing more levodopa to pass the BBB.

Carbidopa

drug that can increase the release of dopamine. This drug can be effective as long as there is a possibility of more dopamine release.

Amantadine

acts as a direct dopamine agonist on dopamine receptor sites in the substantia nigra.

Bromocriptine

oppose the effects of acetylcholine at receptor sites in the substantia nigra.

Anticholinergic drugs

The division of the peripheral nervous system that supply involuntary muscles, glands and other effectors not innervated by the somatic nervous system.

Autonomic nervous system

cranio – sacral outflow

Parasympathetic nervous system (PNS)

“REST AND DIGEST”

In the PNS, the neurotransmitter is

Acetylcholine

There are 2 types of cholinergic receptors

Nicotinic Receptors ○ Muscarinic receptors

thoraco- lumbar outflow

Sympathetic nervous system (SNS)

preganglionic neuron of the SNS

shorter

post ganglionic neuron

longer

Sympathetic nervous system (SNS)

“FIGHT OR FLIGHT”

two neurotransmitters in the SNS

Acetylcholine and Epinephrine and Norepinephrine ( Catecholamines )

Actylcholine is released by the

epinephrine and norepinephrine are the neurotransmitters released by the

post ganglionic neurons

Epinephrine and Norepinephrine may also be called

Adrenalin and Noradrenaline

There are 2 types of adrenergic receptors

○ Alpha receptors ○ Beta receptors

Drugs affecting the PNS are called

Cholinergic Drugs

Drugs affecting the SNS are called

Adrenergic Drugs

directly stimulates the cholinergic receptors to increase its effects

Direct acting cholinergic agonist

indicated for non – obstructive urinary retention like in neurogenic bladder

Bethanechol

indicated for glaucoma, causing pupillary constriction

Carbachol

indicated for glaucoma, causing pupillary constriction

Pilocarpine

– this drug increases acetylcholine effect by inhibiting the action of acetylcholinesterase (an enzyme that removes acetylcholine in the synapse. If acetylcholinesterase is not removed in the synaptic cleft, more acetylcholine stays in the synapse stimulating more receptors, thus enhancing their effects. These drugs are used for treatment of Myasthenia gravis and Alzheimer’s disease’

Indirect acting cholinergic agonist

is an autoimmune disease of the neuromuscular junction (NMJ). This is characterized by destruction of cholinergic receptors at the NMJ that will slow down impulses going to the skeletal muscles. This disease is characterized by the development of muscle weakness and paralysis

MYASTHENIA GRAVIS

To increase junctional transmission, an indirect acting cholinergic agonist inhibits acetylcholinesterase making more acetylcholine present in the junction to improve impulse transmission and muscle function.

anticholinesterase drugs.

short acting anticholinesterase drug used to diagnose the disease. The action lasts for 10 to 20 minutes.

Edrophonium HCL (Tensilon)

long acting anticholinesterase drugs used for therapeutic purposes. The onset of action starts 20 to 30 minutes and may last for 3 – 6 hours.

Neostigmine, Physostigmine, Pyridostigmine

is a degenerative disease of the CNS characterized by loss of neurons in the CNS which may slow down impulse transmission across the synapses of the CNS. One important cause of this is explained by loss of acetylcholine receptors in the postsynaptic neurons, like myasthenia gravis, less receptors mean lesser impulse transmission

ALZHEIMER’S DISEASE

Cholinergic antagonist is also being referred to as an

anticholinergic drug or parasympatholytic.

indicated to decrease secretions, treat bradycardia, pylorospasm, ureteral colic, cause pupil dilation (mydriasis) indicated as preop drug for cataract extraction. Use as antidote for cholinergic crisis

Atropine

use for hyperactive bowel in adults

Dicyclomine

use in motion sickness, indicated to decrease secretion, pupil dilation

Scopolamine

Vascular smooth muscles, iris, visceral smooth muscles like the urinary bladder and iris

Alpha 1 receptors

CNS neurons, pancreatic islets

Alpha 2 receptors

Myocardium, Kidneys, CNS neurons

Beta 1 receptors

Visceral smooth muscles like in the lungs, some vascular smooth muscles, CNS neurons

Beta 2 receptors

these drugs stimulate all adrenergic receptors to enhance their effects

Alpha and Beta adrenergic drugs ( Sympathomimetic drugs )

the drug of choice during CPR, indicated for treatment of shock

Epinephrine

used for treatment of congestive heart failure

Dobutamine

usually given for congestive heart failure and cardiogenic shock

Dopamine

like epinephrine, may be indicated for cardiac arrest

Norepinephrine

these drugs specifically stimulate only the alpha receptors and not the beta receptors

Alpha specific adrenergic agonist

used for treatment of common colds and allergy. This drug causes vasoconstriction to lessen congestion in the nose therefore called decongestants

Phenylephrine

better known for its brand name as Catapres acting on the CNS neurons to decrease norepinephrine flow. This drug is indicated for treatment of hypertension

Clonidine

these drugs specifically stimulate the beta receptors and not the alpha receptors.

Beta specific adrenergic agonist

for treatment of cardiogenic shock and heart block in transplanted hearts.

Isoproterenol

for treatment of obstructive respiratory disease like COPD and bronchial asthma

Salbutamol

these drugs block all adrenergic receptors

Alpha and Beta adrenergic antagonist

these drugs block only the alpha receptors, specific drugs act on the alpha 1 and alpha 2 receptors.

Alpha adrenergic antagonist

more specific drug hypertension in pheochromocytoma, that will have less adverse effects

Phentolamine

these drugs block only the alpha receptors, specific drugs act on the alpha receptors on the blood vessels and urinary bladder to cause vasodilation for treatment of hypertension and bladder emptying for treatment of urinary retention. Although some drugs may act in both blood vessels and urinary bladder at the same time

Alpha 1 selective adrenergic antagonist

these drugs block both beta 1 and beta 2 receptors, particularly affecting both the heart and the lungs, these drugs increase heart rate and bronchoconstriction of the lungs

Beta adrenergic antagonists

These drugs are known teratogenic in animals as

Beta 1 specific adrenergic antagonist

this is a rapid change in the membrane potential that explains how impulses are conducted along the nerves

Action Potential

control of signs and symptoms of the disease

Palliative Treatment

conduction of impulses across the junction between neurons

Synaptic Transmission