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PHARMACOLOGY 1
Pharmacology Question & Answer
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PHARMACOLOGY 2
Pharmacology Question and Answer
1. Hypnotics.
The medications used promote sleep are known as Hypnotics. Hypnotics, also, have an
impact on the central nervous system with the purpose of eliminating and mitigate anxiety which
in return ensures increased sleep with soothing effect. The drugs are known to treat anxiety,
insomnia and panic disorder. There are different types of hypnotics however the main class of
hypnotics is benzodiazepines.
Mechanism of Benzodiazepine Action
The mechanism of Benzodiazepine is considered to be easy since the drug targets GABA
receptors (Chawla 2018). A chloride pathway created in response to sticking together of GABA
which is a neurotransmitter to the receptor. Therefore, the pathways created cause chloride to
flow into the cell making it less receptive to the impact of depolarization. The benzodiazepine
works through the GABA receptors to increase sleep by blocking brainstem monoaminergic
arousal entries. Through the enhancement of VLPO inhibitory GABAergic, the outcomes
provides a forecast of the triggered regions which include the anterior hypothalamus and
brainstem.
Pharmacological Effects
Benzodiazepine compounds are a combination of benzene and diazepine ring. The
combination ensures that the compounds exert anxiolytic, anticonvulsant, sedative, hypnotic and
properties that relax muscles at the targeted receptors. The rate at which benzodiazepine
metabolize varies depending on their different types. For instance, short-acting drugs metabolize
within less than twenty-four hours.
PHARMACOLOGY 3
Indications of Use
Benzodiazepine indication for the treatment of conditions such as anxiety, alcohol
withdrawal, agitation and hyperexcitability among others. The drug reacts in the limbic system
ensuring the gamma-aminobutyric acid has more impact to cause interference with neuron firing.
The reaction leads to an anxiolytic impact when the doses seem lower than required to start
sedation and hypnosis.
Side Effects
The common side effects of benzodiazepines are the depressant effect the drug has on the
central nervous systems. The most common side effects include dizziness, sedation, decreased
alertness, lack of concentration and irritation among others.
Treatment of poisoning
When an overdose occurs, there is need for immediate assessment of the patient. This
includes assessment of breathing, airway, circulation, and monitoring of the patient. However,
cases of benzodiazepine overdose are rare (Gresham 2018).
2. Neuroleptics
Neuroleptics, also referred to as Antipsychotics which are the main tranquilizers used in
psychosis management in schizophrenia and bipolar. Neuroleptics' primary use is the treatment
of people suffering from psychiatric conditions such as bipolar and schizophrenia to ensure that
symptoms control.
Thioxanthenes and butyrophenone Derivatives
PHARMACOLOGY 4
Thioxanthenes derivatives used in the clinical field and psychotherapeutic medication
include Thiothixene, taractan, and clopenthixol. On the other hand, butyrophenone derivatives
include droperidol, haloperidol, and melperone among others.
Pharmacological Effects
Due to various side effects Neuroleptics need to be reserved for use of schizophrenia.
Some of the common the effects include constipation, weight gain, sexual dysfunction due to
hormonal changes and sleeplessness among others.
Mechanism of Action
The hindrance of dopamine D2 receptors in the central nervous system is the reaction of
in the first generation neuroleptic therapies. However, the second generation of neuroleptics is
different because they transiently occupy D2 receptors and quickly desalinate for normal
dopamine neurotransmission. Second generation neuroleptics also contain antagonistic effects on
5HT2A receptors (Gossman 2019).
Indications for Use
Neuroleptics are used for treatment and managing psychiatric disorders. Neuroleptics
categorization is into two classifications of the first-generation and second generation.
Side Effects and their Prevention
There are different side effects of neuroleptics, which are based on the first and the
second generation classification. They caused increased sedation and sexual dysfunction.
Neuroleptics also lead to postural hypotension, sudden cardiac death, and cardiac arrhythmia
among others. For medical personnel to prevent these side effects it is essential that they
PHARMACOLOGY 5
understand profiles of the medications. Additionally, treatment dosage should be adjusted in case
of adverse side effects to avoid complications (Muench 2010).
3. General Anesthetics
General anesthesia is the process through which a combination of various general
anesthetic agents is administrated in order to attain different results. For instance, analgesia,
amnesia, and unconsciousness among others. General anesthesia can be administered
intravenously or through a gas mask, and there is a possibility of using both methods
simultaneously. However general anesthesia is not used during all medical procedures due to the
high risk associated with the process. When under general anesthesia, the patient no more
extended breath on their own hence they are put under special breathing equipment (Karch
2017).
Drugs for Non-inhalation Anesthesia comparative Characteristics of the Individual
Drugs
There different classes of drugs used during general anesthesia. The drugs include
barbiturate and nonbarbiturate anesthetics, gas anesthetics, and volatile liquids. The focus in this
section is on drugs that are non-inhalation during the process of anesthetics. To start with are the
barbiturate anesthetics, which are administered through intravenous to provide quick anesthesia.
Methohexital is the only drug that is classified under barbiturate anesthetics. The drug has quick
mechanism action with a recovery period of approximately three to four minutes. The drug is
considered to be lipophilic hence dissolves quickly through the lipid blood-brain diffusing into
the brain. Nonbarbiturate drugs are also used in intravenous administration (Karch 2017). The
drugs categories include droperidol, etomidate, and ketamine among others. The non-barbiturate
PHARMACOLOGY 6
drugs react in the reticular and limbic system to increase the impact of gamma-aminobutyric
acid.
Features of actions
Methohexital is classified under barbiturate and has no analgesic effects; hence, the
patients need postoperative analgesics. On the other hand, midazolam is considered to be highly
amnesiac hence used for amnesia. Drugs such as droperidol cause mental detachment, sedation,
and decreases vomiting and nausea.
Indications for Use
General anesthetics agents are used to causing analgesia, unconsciousness, and loss of
pain for patients during surgical procedures, amnesia, and loss of the ability to recognize one’s
surroundings. Additionally, the drugs are used in ensuring that the body’s reflexes are obstructed
which prevents involuntary reaction of reflex to injury.
Side effects
Barbiturate drugs are associated with have a connection to the suppression of the central
nervous system. This includes reduced pulse, reduced gastrointestinal activity, hypotension and
repression of respirations (Karch 2017). During the process of recovery nausea and vomiting are
some of the commonly seen effects. On the other hand, nonbarbiturate drugs cause skin
breakdown due to lack of movement. Drugs such as ketamine can lead to hallucinations and
psychotic behaviors. Droperidol can also cause drowsiness and chills.
4. Neuroleptics – Phenothiazine
PHARMACOLOGY 7
Neuroleptics are also referred to as antipsychotics. Phenothiazine neuroleptics are
medications that are primary used for the treatment and managing of psychotic disorders and
schizophrenia. However, there are types of phenothiazine used for treatment of vomiting, nausea,
and hiccups (Karch 2017). Some of the phenothiazine neuroleptics include chlorpromazine,
fluphenazine, perphenazine, and prochlorperazine among others.
Mechanism of Action
Phenothiazine creates a barrier for dopamine receptors hence preventing stimulation of
postsynaptic neurons by dopamine. The drugs contain blocking impact due to anticholinergic,
antihistamine, and alpha-adrenergic which initiate prevention of dopamine receptor regions
(Karch 2017). The drugs also lower reticular activating systems causing the reduction of stimuli
flows into the brain.
Pharmacological Effects
The drugs lack consistent absorption from the gastrointestinal tract. This mainly depends
on the drug and the method of preparation used. Neuroleptics have a wide distribution in the
tissues where they are also stored. After drug use is terminated, the drugs continue release from
the tissues up to six months. Neuroleptics are metabolized in the liver and excretion takes place
through urine and bile. For pregnant women and nursing mothers neuroleptics flow through the
placenta entering breast milk.
Indications of Use
Neuroleptics are indicated for schizophrenia and other psychotic disorders, which include
combative behavior, hyperactivity, and severe behavioral issues in children. Apart from being
used for emotional disorders, phenothiazine also controls agitation, severe vomiting and nausea,
PHARMACOLOGY 8
and reduce pain for patients (Ogbru 2018). Drugs such as chlorpromazine are used in
combination with other drugs for treatment of types of porphyria and tetanus in some cases.
Side Effects and their Prevention
There are different side effects caused by phenothiazine neuroleptics. The most
commonly identified side effects include drowsiness, low blood pressure, headache, and blurred
vision (Karch 2017). The adverse effects of the neuroleptics are those caused through the
blocking of dopamine, anticholinergic, and alpha-adrenergic activities. For instance, due to
dopamine blockage there is increased level of prolactin, which leads to gynecomastia. In order to
prevent the side effects, patients using the drugs should be highly monitored to determine
changes of dosage and side effects.
5. Non-narcotic Analgesics
Non-narcotic analgesics are drugs administered during the treatment and control of
pain and inflammation. The non-narcotic analgesic drugs and therapies also are applicable
during process of surgical procedures to eliminate pain (Leitnar 2016). Drug such as aspirin
is commonly used Non-narcotic agent for pain control. Non-narcotic analgesics initially were
known as non-opioid. The commonly used nonopioid analgesics include tramadol, clonidine,
ziconotide, and dexmedetomidine.
Classification According to Chemical Structure and Selectivity for COX
Non-narcotic analgesics also include nonsteroidal anti-inflammatory medications,
selective COX-2 inhibitors, and acetaminophen. Non-steroidal anti-inflammatory drugs
prevent cyclooxygenases COX-1 and COX-2 hence temper with the creation of prostaglandin
which is an essential conciliator of inflammation and pain. Additionally, non-steroidal anti-
PHARMACOLOGY 9
inflammatory drugs contain antipyretic, anti-inflammatory impacts and analgesic for pain
management (Burchum 2019). COX 1 and COX2 are isozymes of cyclooxygenase. COX 1 is
activated through physiological stimuli while COX 2 is activated through inflammation
stimuli. Selective COX2 inhibitors are contained similar impact as those of non-steroidal
anti-inflammatory drugs however indicate reduced risk for gastrointestinal effects.
Mechanism of Action
Mechanism of action for non-steroidal anti-inflammatory drugs is reversible
hindering of COX 1, and COX 2 reduces prostaglandin synthesis. The movement of non-
narcotic analgesics into the blood-brain barrier with secondary inhibition of nociceptive
stimuli commences flow of prostaglandins at the central nervous system level and spinal
cord.
Indication for Use
The indication of non-narcotic analgesics is for acute and chronic pain. The drugs are also
used in combination with other medications and therapies for treating pain and other disorders.
Side Effects
Some of the possible side effects of the medication include nausea, vomiting, constipation,
and anxiety (Burchum 2019). Some of the adverse side effects include kidney problems and
liver problems. Non-steroidal anti-inflammatory drugs can cause renal function impairment,
which affects the kidney. Selective COX 2 inhibitors can increase the risk of heart problems and
stroke. To prevent the side effects patients should be monitored. Patients with allergic reactions
to NSAIDs should use alternative medicine.
PHARMACOLOGY 10
6. Narcotic (Opioid) Analgesics
Narcotic analgesics are drugs with similar reactions to those of morphine. The term
opioid is derived from opium, which includes different agents such as codeine, oxycodone,
fentanyl, and morphine. Additionally, narcotic medications are unique based on the type of
opioid receptor with which they react.
Mechanism of Analgesic Effect
Primary narcotic analgesic agents relieve pain by copying the actions of endogenous
opioid peptides. Morphine drugs and opioid peptides have similar structural systems. The
analgesic action of opioid peptides and morphine drugs can be hindered by similar antagonist
naloxone.
The central and peripheral actions taking place can lead morphine to cause respiratory
depression, retention of urine, cough suppression and constipation among others. If drug use is
over a long period then there is possibility of tolerance and physical dependence. Additionally,
some central and peripheral effect such as respiratory depression is detrimental to patients.
Side Effects
There different side effects from the use of opioids. Prolonged use of the medications
leads to shifts in hormonal balance hence changing the immune functionality. Hormonal
fluctuations due to the use of drugs can cause increased levels of prolactin and reduce luteinizing
hormone levels. Other commonly identified side effects include nausea, vomiting, constipation,
and dizziness among others (Burchum 2019).
PHARMACOLOGY 11
Overdose of the medication can lead to signs such as coma and respiratory depression.
Additionally, blood pressure may be lowered due to hypoxia, which, if prolonged, leads to
shock. In the case of acute poisoning treatment includes ventilator support and administering
opioid antagonists. The best-considered antagonist for treatment is naloxone.
7. Anxiolytics – Benzodiazepine Tranquilizers
Anxiolytics are medications used to depress the central nervous system hence reducing
and controlling anxiety. Benzodiazepine is a drug that used to treat anxiety through increase of
GABA reaction. Benzodiapine controls anxiety disorders without causing sedation or physical
dependency. Some of the benzodiapine include alprazolam, chlordiazepoxide, clonazepam, and
lorazepam among others.
Benzodiazepine reacts in the limbic system and reticular activating system to produce
gamma-aminobutyric acid making more effective to cause alteration with neuron release.
Therefore gamma-aminobutyric acid produced ensures the postsynaptic cell is stabilized.
Additionally, benzodiapine utilized for therapies of anxiety conditions, alcohol withdrawal,
agitation, and hyperexcitability.
Benzodiazepines begins to soak up in the gastrointestinal tract where the highest levels
are attained in approximately two hours. The drugs diffuse swiftly into the body with metabolism
taking place in the liver. The drug needs to be given in lower doses in regards to patients which
liver complications.
The common toxic impact of the medication include drowsiness, constipation, vomiting,
and nausea among others. However, effects on the central and peripheral systems lead to
sedation, depression, blurred vision, and amnesia. The genitourinary impact is signed, such as
PHARMACOLOGY 12
urinary retention and shifts in sexual functionality. Toxicity signs are similar to pretreatment
symptoms; therefore, drug should be used with great caution and monitoring from physician.
8. General Anesthetics
General anesthetic involves the use of different agents with the aim of analgesia, reducing
pain, amnesia, and loss of awareness. General anesthesia enables medical professionals to reduce
any risks to the patient and increase the safety and comfort of the patient. Inhalation anesthetic is
mainly used to initiate and manage general anesthesia and sedation.
Inhalation anesthetic is classified into two categories. These include gases and volatile
liquids whereby gases are in gaseous state and volatile are in liquid state. Anesthetic gases
include nitrous oxide, while the volatile liquids include enflurane, isoflurane, sevoflurane, and
desflurane.
The different stages of general anesthesia include induction, maintenance, and recovery.
Nitrous oxide is used for analgesia because it rushes in the body; however, it cannot cause
muscle relaxation. The gas has quick action hence rapid recovery. Side effects caused by nitrous
oxide include hypoxia, chest pain, and stroke. When using desflurane there is possibility of high
sensitivity hence should not be used on patients with respiratory complications.
9. Antidepressants
Antidepressants are medications therapies for depression, anxiety, dysthymia, and
chronic depression. Depression is a disorder with changes in mood and loss of excitement in life
with feelings of sadness and worthlessness. An antidepressant that is available for depression
treatment is classified into five main categories. These include selective serotonin reuptake
PHARMACOLOGY 13
inhibitors, serotonin or norepinephrine reuptake inhibitors, tricyclic antidepressants, monoamine
oxidize inhibitors and atypical antidepressants.
There are different side effects that are commonly identified with the use of
antidepressant. For instance, antidepressants can cause sexual problems such as impotence and
decreased sexual interest. Use of these drugs can also lead to weight gain however, in the initial
stages of use there can be weight loss due to vomiting and nausea. Abrupt discontinuation use of
the drugs can lead to withdrawal symptoms such as dizziness, headache, nausea, and anxiety.
The toxicity of some of the antidepressants can be highly harmful to the patient. Additionally,
patients with symptoms of suicidal feelings should not be given more than a weekly dose.
10. Atypical Antipsychotics
Atypical antipsychotics are the second-generation antipsychotic drugs. Clozapine is the
primary drug that is classified under the atypical antipsychotic drugs. These are the most
effective medication therapies for schizophrenia. However the drug causes agranulocytosis; there
should not be used in patients that can use alternative medicine.
The mechanism action of atypical antipsychotic drugs is the blocking of receptors for
dopamine and serotonin. Even with the profound effects of clozapine of blocking receptors solid
blockade is on 5-HT2 receptors. On the other hand, toxicity impact of the drug include weight
gain, orthostatic hypotension, dry mouth, blurred vision, urinary retention, and constipation. The
drugs can also cause seizures hence patients should not drive while under treatment.
PHARMACOLOGY 14
Bibliography
Burchum, J, 2019, Lehne’s Pharmacology for Nursing Care, 10th
ed, Missouri: Elsevier
Inc.
Chawla, J, 2018, What are the Mechanisms of Action of Benzodiazepines and
Benzodiazepines Receptors Agonists for Insomnia, Medscape.
https://www.medscape.com/answers/1187829-70503/what-are-the-mechanisms-
of-action-of-benzodiazepines-and-benzodiazepine-receptor-agonists-for-insomnia
Gresham, C, 2018, Benzodiazepine Toxicity Treatment and Management, Medscape.
https://emedicine.medscape.com/article/813255-treatment
Gossman, W, et al. 2019, Neuroleptic Medications, NCBI Journals,
https://www.ncbi.nlm.nih.gov/books/NBK459150/#_ncbi_dlg_citbx_NBK459150
Karch, A, 2017, Focus on Nursing Pharmacology, 7th
Ed. China: Lippincott Williams &
Wilkins, Wolters Kluwer.
Leitnar, j, 2016, Non-narcotic Analgesics for Musculoskeletal Pain, Clinical Advisor.
https://www.clinicaladvisor.com/home/consultations/non-narcotic-analgesics-for-
musculoskeletal-pain/
Muench, J, 2010, Adverse Effects of Antipsychotic Medications, American Family
Physician, vol. 81, no. 5, pp. 617-622.
https://www.aafp.org/afp/2010/0301/p617.html
Ogbru, O, 2018, Phenothiazine Antipsychotics, MedicineNet.
https://www.medicinenet.com/phenothiazines-oral/article.htm

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Pharmacology q-&-a

  • 1. PHARMACOLOGY 1 Pharmacology Question & Answer Author’s Name Course Tutor Institution Date
  • 2. PHARMACOLOGY 2 Pharmacology Question and Answer 1. Hypnotics. The medications used promote sleep are known as Hypnotics. Hypnotics, also, have an impact on the central nervous system with the purpose of eliminating and mitigate anxiety which in return ensures increased sleep with soothing effect. The drugs are known to treat anxiety, insomnia and panic disorder. There are different types of hypnotics however the main class of hypnotics is benzodiazepines. Mechanism of Benzodiazepine Action The mechanism of Benzodiazepine is considered to be easy since the drug targets GABA receptors (Chawla 2018). A chloride pathway created in response to sticking together of GABA which is a neurotransmitter to the receptor. Therefore, the pathways created cause chloride to flow into the cell making it less receptive to the impact of depolarization. The benzodiazepine works through the GABA receptors to increase sleep by blocking brainstem monoaminergic arousal entries. Through the enhancement of VLPO inhibitory GABAergic, the outcomes provides a forecast of the triggered regions which include the anterior hypothalamus and brainstem. Pharmacological Effects Benzodiazepine compounds are a combination of benzene and diazepine ring. The combination ensures that the compounds exert anxiolytic, anticonvulsant, sedative, hypnotic and properties that relax muscles at the targeted receptors. The rate at which benzodiazepine metabolize varies depending on their different types. For instance, short-acting drugs metabolize within less than twenty-four hours.
  • 3. PHARMACOLOGY 3 Indications of Use Benzodiazepine indication for the treatment of conditions such as anxiety, alcohol withdrawal, agitation and hyperexcitability among others. The drug reacts in the limbic system ensuring the gamma-aminobutyric acid has more impact to cause interference with neuron firing. The reaction leads to an anxiolytic impact when the doses seem lower than required to start sedation and hypnosis. Side Effects The common side effects of benzodiazepines are the depressant effect the drug has on the central nervous systems. The most common side effects include dizziness, sedation, decreased alertness, lack of concentration and irritation among others. Treatment of poisoning When an overdose occurs, there is need for immediate assessment of the patient. This includes assessment of breathing, airway, circulation, and monitoring of the patient. However, cases of benzodiazepine overdose are rare (Gresham 2018). 2. Neuroleptics Neuroleptics, also referred to as Antipsychotics which are the main tranquilizers used in psychosis management in schizophrenia and bipolar. Neuroleptics' primary use is the treatment of people suffering from psychiatric conditions such as bipolar and schizophrenia to ensure that symptoms control. Thioxanthenes and butyrophenone Derivatives
  • 4. PHARMACOLOGY 4 Thioxanthenes derivatives used in the clinical field and psychotherapeutic medication include Thiothixene, taractan, and clopenthixol. On the other hand, butyrophenone derivatives include droperidol, haloperidol, and melperone among others. Pharmacological Effects Due to various side effects Neuroleptics need to be reserved for use of schizophrenia. Some of the common the effects include constipation, weight gain, sexual dysfunction due to hormonal changes and sleeplessness among others. Mechanism of Action The hindrance of dopamine D2 receptors in the central nervous system is the reaction of in the first generation neuroleptic therapies. However, the second generation of neuroleptics is different because they transiently occupy D2 receptors and quickly desalinate for normal dopamine neurotransmission. Second generation neuroleptics also contain antagonistic effects on 5HT2A receptors (Gossman 2019). Indications for Use Neuroleptics are used for treatment and managing psychiatric disorders. Neuroleptics categorization is into two classifications of the first-generation and second generation. Side Effects and their Prevention There are different side effects of neuroleptics, which are based on the first and the second generation classification. They caused increased sedation and sexual dysfunction. Neuroleptics also lead to postural hypotension, sudden cardiac death, and cardiac arrhythmia among others. For medical personnel to prevent these side effects it is essential that they
  • 5. PHARMACOLOGY 5 understand profiles of the medications. Additionally, treatment dosage should be adjusted in case of adverse side effects to avoid complications (Muench 2010). 3. General Anesthetics General anesthesia is the process through which a combination of various general anesthetic agents is administrated in order to attain different results. For instance, analgesia, amnesia, and unconsciousness among others. General anesthesia can be administered intravenously or through a gas mask, and there is a possibility of using both methods simultaneously. However general anesthesia is not used during all medical procedures due to the high risk associated with the process. When under general anesthesia, the patient no more extended breath on their own hence they are put under special breathing equipment (Karch 2017). Drugs for Non-inhalation Anesthesia comparative Characteristics of the Individual Drugs There different classes of drugs used during general anesthesia. The drugs include barbiturate and nonbarbiturate anesthetics, gas anesthetics, and volatile liquids. The focus in this section is on drugs that are non-inhalation during the process of anesthetics. To start with are the barbiturate anesthetics, which are administered through intravenous to provide quick anesthesia. Methohexital is the only drug that is classified under barbiturate anesthetics. The drug has quick mechanism action with a recovery period of approximately three to four minutes. The drug is considered to be lipophilic hence dissolves quickly through the lipid blood-brain diffusing into the brain. Nonbarbiturate drugs are also used in intravenous administration (Karch 2017). The drugs categories include droperidol, etomidate, and ketamine among others. The non-barbiturate
  • 6. PHARMACOLOGY 6 drugs react in the reticular and limbic system to increase the impact of gamma-aminobutyric acid. Features of actions Methohexital is classified under barbiturate and has no analgesic effects; hence, the patients need postoperative analgesics. On the other hand, midazolam is considered to be highly amnesiac hence used for amnesia. Drugs such as droperidol cause mental detachment, sedation, and decreases vomiting and nausea. Indications for Use General anesthetics agents are used to causing analgesia, unconsciousness, and loss of pain for patients during surgical procedures, amnesia, and loss of the ability to recognize one’s surroundings. Additionally, the drugs are used in ensuring that the body’s reflexes are obstructed which prevents involuntary reaction of reflex to injury. Side effects Barbiturate drugs are associated with have a connection to the suppression of the central nervous system. This includes reduced pulse, reduced gastrointestinal activity, hypotension and repression of respirations (Karch 2017). During the process of recovery nausea and vomiting are some of the commonly seen effects. On the other hand, nonbarbiturate drugs cause skin breakdown due to lack of movement. Drugs such as ketamine can lead to hallucinations and psychotic behaviors. Droperidol can also cause drowsiness and chills. 4. Neuroleptics – Phenothiazine
  • 7. PHARMACOLOGY 7 Neuroleptics are also referred to as antipsychotics. Phenothiazine neuroleptics are medications that are primary used for the treatment and managing of psychotic disorders and schizophrenia. However, there are types of phenothiazine used for treatment of vomiting, nausea, and hiccups (Karch 2017). Some of the phenothiazine neuroleptics include chlorpromazine, fluphenazine, perphenazine, and prochlorperazine among others. Mechanism of Action Phenothiazine creates a barrier for dopamine receptors hence preventing stimulation of postsynaptic neurons by dopamine. The drugs contain blocking impact due to anticholinergic, antihistamine, and alpha-adrenergic which initiate prevention of dopamine receptor regions (Karch 2017). The drugs also lower reticular activating systems causing the reduction of stimuli flows into the brain. Pharmacological Effects The drugs lack consistent absorption from the gastrointestinal tract. This mainly depends on the drug and the method of preparation used. Neuroleptics have a wide distribution in the tissues where they are also stored. After drug use is terminated, the drugs continue release from the tissues up to six months. Neuroleptics are metabolized in the liver and excretion takes place through urine and bile. For pregnant women and nursing mothers neuroleptics flow through the placenta entering breast milk. Indications of Use Neuroleptics are indicated for schizophrenia and other psychotic disorders, which include combative behavior, hyperactivity, and severe behavioral issues in children. Apart from being used for emotional disorders, phenothiazine also controls agitation, severe vomiting and nausea,
  • 8. PHARMACOLOGY 8 and reduce pain for patients (Ogbru 2018). Drugs such as chlorpromazine are used in combination with other drugs for treatment of types of porphyria and tetanus in some cases. Side Effects and their Prevention There are different side effects caused by phenothiazine neuroleptics. The most commonly identified side effects include drowsiness, low blood pressure, headache, and blurred vision (Karch 2017). The adverse effects of the neuroleptics are those caused through the blocking of dopamine, anticholinergic, and alpha-adrenergic activities. For instance, due to dopamine blockage there is increased level of prolactin, which leads to gynecomastia. In order to prevent the side effects, patients using the drugs should be highly monitored to determine changes of dosage and side effects. 5. Non-narcotic Analgesics Non-narcotic analgesics are drugs administered during the treatment and control of pain and inflammation. The non-narcotic analgesic drugs and therapies also are applicable during process of surgical procedures to eliminate pain (Leitnar 2016). Drug such as aspirin is commonly used Non-narcotic agent for pain control. Non-narcotic analgesics initially were known as non-opioid. The commonly used nonopioid analgesics include tramadol, clonidine, ziconotide, and dexmedetomidine. Classification According to Chemical Structure and Selectivity for COX Non-narcotic analgesics also include nonsteroidal anti-inflammatory medications, selective COX-2 inhibitors, and acetaminophen. Non-steroidal anti-inflammatory drugs prevent cyclooxygenases COX-1 and COX-2 hence temper with the creation of prostaglandin which is an essential conciliator of inflammation and pain. Additionally, non-steroidal anti-
  • 9. PHARMACOLOGY 9 inflammatory drugs contain antipyretic, anti-inflammatory impacts and analgesic for pain management (Burchum 2019). COX 1 and COX2 are isozymes of cyclooxygenase. COX 1 is activated through physiological stimuli while COX 2 is activated through inflammation stimuli. Selective COX2 inhibitors are contained similar impact as those of non-steroidal anti-inflammatory drugs however indicate reduced risk for gastrointestinal effects. Mechanism of Action Mechanism of action for non-steroidal anti-inflammatory drugs is reversible hindering of COX 1, and COX 2 reduces prostaglandin synthesis. The movement of non- narcotic analgesics into the blood-brain barrier with secondary inhibition of nociceptive stimuli commences flow of prostaglandins at the central nervous system level and spinal cord. Indication for Use The indication of non-narcotic analgesics is for acute and chronic pain. The drugs are also used in combination with other medications and therapies for treating pain and other disorders. Side Effects Some of the possible side effects of the medication include nausea, vomiting, constipation, and anxiety (Burchum 2019). Some of the adverse side effects include kidney problems and liver problems. Non-steroidal anti-inflammatory drugs can cause renal function impairment, which affects the kidney. Selective COX 2 inhibitors can increase the risk of heart problems and stroke. To prevent the side effects patients should be monitored. Patients with allergic reactions to NSAIDs should use alternative medicine.
  • 10. PHARMACOLOGY 10 6. Narcotic (Opioid) Analgesics Narcotic analgesics are drugs with similar reactions to those of morphine. The term opioid is derived from opium, which includes different agents such as codeine, oxycodone, fentanyl, and morphine. Additionally, narcotic medications are unique based on the type of opioid receptor with which they react. Mechanism of Analgesic Effect Primary narcotic analgesic agents relieve pain by copying the actions of endogenous opioid peptides. Morphine drugs and opioid peptides have similar structural systems. The analgesic action of opioid peptides and morphine drugs can be hindered by similar antagonist naloxone. The central and peripheral actions taking place can lead morphine to cause respiratory depression, retention of urine, cough suppression and constipation among others. If drug use is over a long period then there is possibility of tolerance and physical dependence. Additionally, some central and peripheral effect such as respiratory depression is detrimental to patients. Side Effects There different side effects from the use of opioids. Prolonged use of the medications leads to shifts in hormonal balance hence changing the immune functionality. Hormonal fluctuations due to the use of drugs can cause increased levels of prolactin and reduce luteinizing hormone levels. Other commonly identified side effects include nausea, vomiting, constipation, and dizziness among others (Burchum 2019).
  • 11. PHARMACOLOGY 11 Overdose of the medication can lead to signs such as coma and respiratory depression. Additionally, blood pressure may be lowered due to hypoxia, which, if prolonged, leads to shock. In the case of acute poisoning treatment includes ventilator support and administering opioid antagonists. The best-considered antagonist for treatment is naloxone. 7. Anxiolytics – Benzodiazepine Tranquilizers Anxiolytics are medications used to depress the central nervous system hence reducing and controlling anxiety. Benzodiazepine is a drug that used to treat anxiety through increase of GABA reaction. Benzodiapine controls anxiety disorders without causing sedation or physical dependency. Some of the benzodiapine include alprazolam, chlordiazepoxide, clonazepam, and lorazepam among others. Benzodiazepine reacts in the limbic system and reticular activating system to produce gamma-aminobutyric acid making more effective to cause alteration with neuron release. Therefore gamma-aminobutyric acid produced ensures the postsynaptic cell is stabilized. Additionally, benzodiapine utilized for therapies of anxiety conditions, alcohol withdrawal, agitation, and hyperexcitability. Benzodiazepines begins to soak up in the gastrointestinal tract where the highest levels are attained in approximately two hours. The drugs diffuse swiftly into the body with metabolism taking place in the liver. The drug needs to be given in lower doses in regards to patients which liver complications. The common toxic impact of the medication include drowsiness, constipation, vomiting, and nausea among others. However, effects on the central and peripheral systems lead to sedation, depression, blurred vision, and amnesia. The genitourinary impact is signed, such as
  • 12. PHARMACOLOGY 12 urinary retention and shifts in sexual functionality. Toxicity signs are similar to pretreatment symptoms; therefore, drug should be used with great caution and monitoring from physician. 8. General Anesthetics General anesthetic involves the use of different agents with the aim of analgesia, reducing pain, amnesia, and loss of awareness. General anesthesia enables medical professionals to reduce any risks to the patient and increase the safety and comfort of the patient. Inhalation anesthetic is mainly used to initiate and manage general anesthesia and sedation. Inhalation anesthetic is classified into two categories. These include gases and volatile liquids whereby gases are in gaseous state and volatile are in liquid state. Anesthetic gases include nitrous oxide, while the volatile liquids include enflurane, isoflurane, sevoflurane, and desflurane. The different stages of general anesthesia include induction, maintenance, and recovery. Nitrous oxide is used for analgesia because it rushes in the body; however, it cannot cause muscle relaxation. The gas has quick action hence rapid recovery. Side effects caused by nitrous oxide include hypoxia, chest pain, and stroke. When using desflurane there is possibility of high sensitivity hence should not be used on patients with respiratory complications. 9. Antidepressants Antidepressants are medications therapies for depression, anxiety, dysthymia, and chronic depression. Depression is a disorder with changes in mood and loss of excitement in life with feelings of sadness and worthlessness. An antidepressant that is available for depression treatment is classified into five main categories. These include selective serotonin reuptake
  • 13. PHARMACOLOGY 13 inhibitors, serotonin or norepinephrine reuptake inhibitors, tricyclic antidepressants, monoamine oxidize inhibitors and atypical antidepressants. There are different side effects that are commonly identified with the use of antidepressant. For instance, antidepressants can cause sexual problems such as impotence and decreased sexual interest. Use of these drugs can also lead to weight gain however, in the initial stages of use there can be weight loss due to vomiting and nausea. Abrupt discontinuation use of the drugs can lead to withdrawal symptoms such as dizziness, headache, nausea, and anxiety. The toxicity of some of the antidepressants can be highly harmful to the patient. Additionally, patients with symptoms of suicidal feelings should not be given more than a weekly dose. 10. Atypical Antipsychotics Atypical antipsychotics are the second-generation antipsychotic drugs. Clozapine is the primary drug that is classified under the atypical antipsychotic drugs. These are the most effective medication therapies for schizophrenia. However the drug causes agranulocytosis; there should not be used in patients that can use alternative medicine. The mechanism action of atypical antipsychotic drugs is the blocking of receptors for dopamine and serotonin. Even with the profound effects of clozapine of blocking receptors solid blockade is on 5-HT2 receptors. On the other hand, toxicity impact of the drug include weight gain, orthostatic hypotension, dry mouth, blurred vision, urinary retention, and constipation. The drugs can also cause seizures hence patients should not drive while under treatment.
  • 14. PHARMACOLOGY 14 Bibliography Burchum, J, 2019, Lehne’s Pharmacology for Nursing Care, 10th ed, Missouri: Elsevier Inc. Chawla, J, 2018, What are the Mechanisms of Action of Benzodiazepines and Benzodiazepines Receptors Agonists for Insomnia, Medscape. https://www.medscape.com/answers/1187829-70503/what-are-the-mechanisms- of-action-of-benzodiazepines-and-benzodiazepine-receptor-agonists-for-insomnia Gresham, C, 2018, Benzodiazepine Toxicity Treatment and Management, Medscape. https://emedicine.medscape.com/article/813255-treatment Gossman, W, et al. 2019, Neuroleptic Medications, NCBI Journals, https://www.ncbi.nlm.nih.gov/books/NBK459150/#_ncbi_dlg_citbx_NBK459150 Karch, A, 2017, Focus on Nursing Pharmacology, 7th Ed. China: Lippincott Williams & Wilkins, Wolters Kluwer. Leitnar, j, 2016, Non-narcotic Analgesics for Musculoskeletal Pain, Clinical Advisor. https://www.clinicaladvisor.com/home/consultations/non-narcotic-analgesics-for- musculoskeletal-pain/ Muench, J, 2010, Adverse Effects of Antipsychotic Medications, American Family Physician, vol. 81, no. 5, pp. 617-622. https://www.aafp.org/afp/2010/0301/p617.html Ogbru, O, 2018, Phenothiazine Antipsychotics, MedicineNet. https://www.medicinenet.com/phenothiazines-oral/article.htm