AMU PHARMACOLOGY INDIVIDUAL

ASSISMENT FOR 2015 BATCH

RADIOLOGY STUDENT

BIRHANU CHALIE ID: NSR/521/15

SUBMISSION DATE :27/01/2017 E.C

SUBMITTED TO: TEWODROS
AGEDAW(MSC)

TABLE CONTENT

1.Explain the pharmacological aspects of general anesthesia.

2.Discuss the different categories of anticancer drugs.
3.Describe the therapeutic uses of steroid hormones.
4.Explain the mechanism of action of hormonal contraceptives and list the
different types.
 5.Discuss the pharmacology of antiprotozoal medications

1.the pharmacological aspects of

general anesthesia.
INTRODUCTION ABOUT GENERAL
ANESTHESIA DRUG

General anesthesia drugs are essential

components used to induce a state of
controlled unconsciousness during
surgical procedures. These medications
work by interrupting nerve signals in the
brain and body, preventing the sensation
of pain and memory formation during
surgery. The administration of these
drugs is typically performed by an
anesthesiologist or a certified nurse
anesthetist, who monitors the patient’s
vital signs throughout the procedure to
ensure safety and effectiveness.
▰ 1.2 TYPES OF GENERAL
ANSTHESIA DRUGS
1.Induction agent
2. Inhalational anesthesia
3.Muscle relaxant
4. Adjuvant
 5.Reversal agent
1.Induction agent
Induction agents are a class of drugs
utilized to initiate and maintain general
anesthesia during surgical procedures.
These agents can be administered
intravenously or through inhalation,
although the term typically refers to
intravenous agents. The primary
purpose of these agents is to induce a
state of unconsciousness and analgesia
in patients, allowing for painless surgical
interventions.
1.Common Induction Agents
Propofol
Mechanism: Propofol works
primarily by activating GABA receptors,
which enhances inhibitory
neurotransmission in the central nervous
system.
Indication: It is commonly
used for induction and maintenance of
general anesthesia.
Dosing: Typical dosing ranges
from 1-2.5 mg/kg for induction and 50-
150 mcg/kg/min for maintenance.
 Considerations: While well-tolerated, it
can cause hypotension and respiratory
depression. It does not provide
analgesia, necessitating concurrent
opioid administration.
2.Ketamine
 Mechanism: Ketamine acts by both
activating GABA receptors and inhibiting
NMDA receptors, leading to dissociative
anesthesia.
 Indication: Primarily used for induction
in patients who may not tolerate other
agents due to their hemodynamic
effects.
 Dosing: Dosing ranges from 0.5-2
mg/kg for induction.
 Considerations: It can cause
hallucinations and agitation upon
emergence but has minimal respiratory
effects, making it suitable for asthmatic
patients.
3.Thiopentone
 Mechanism: Thiopentone also activates
GABA receptors but is less commonly
used today due to the availability of
newer agents.
 Indication: Used mainly as an induction
bolus rather than continuous infusion.
 Considerations: It provides rapid onset
but can lead to cardiovascular
depression.
 4.Etomidate
Mechanism: Like Propofol and
Thiopentone, Etomidate activates GABA
receptors.
 Indication: Often chosen for patients at
risk of cardiovascular instability since it
has minimal hemodynamic effects.
 Dosing: Typical dosing is between 0.2-
0.6 mg/kg.
 Considerations: It may cause adrenal
suppression if used long-term and can
increase postoperative nausea.
5.Midazolam
Mechanism: As a
benzodiazepine, Midazolam enhances
the effect of GABA at the GABA-A
receptor.
 Indication: Used both as an induction
agent and as premedication due to its
anxiolytic properties.
 Dosing: Dosing varies based on use;
typically around 0.1-0.3 mg/kg for
induction.
 Considerations: It provides sedation
but requires careful monitoring due to
potential respiratory depression.
Clinical Use and Selection of
Induction Agents
The choice of an appropriate induction
agent depends on various factors
including patient health status, type of
surgery, anticipated hemodynamic
changes, and specific contraindications
related to each drug’s profile. For
instance
Patients with cardiovascular issues may
benefit from Etomidate or Ketamine due
to their favorable hemodynamic profile
Propofol might be avoided in
hypovolemic patients because it
significantly lowers blood pressure.
1.3 Inhalational anesthesia
Inhalational anesthesia refers to the use
of chemical compounds that possess
general anesthetic properties, delivered
through inhalation. These agents are
typically administered via a face mask,
laryngeal mask airway, or tracheal tube
connected to an anesthetic vaporizer
and delivery system. The primary goal is
to induce a state of unconsciousness and
immobility during surgical procedures.
Current Agents
The most commonly used inhalational
anesthetics today include volatile agents
such as isoflurane, sevoflurane, and
desflurane, along with gases like nitrous
oxide and xenon. Each agent has unique
characteristics regarding potency, onset
time, and side effects.
Mechanism of Action
The exact mechanism by which inhaled
anesthetics produce their effects
remains largely unknown. However, it is
believed that they act on multiple
molecular targets within the central
nervous system. They enhance inhibitory
ion channels’ function while blocking
excitatory ones, leading to overall
central nervous system depression.
Pharmacokinetics
The pharmacokinetics of inhalational
anesthetics involves their absorption
from the alveoli into systemic circulation,
distribution throughout the body, and
eventual elimination primarily through
the lungs. The effectiveness of these
agents can be measured using the
minimum alveolar concentration (MAC),
which indicates the dose required to
prevent movement in response to
surgical stimuli in 50% of patients.
Historical Context
The history of inhalational anesthesia
dates back to the 19th century when
nitrous oxide was first used for dental
procedures by Horace Wells in 1844.
This was followed by the introduction of
ether and chloroform for surgical
anesthesia. Over time, advancements in
chemistry led to the development of
modern halogenated volatile anesthetics
that are safer and more effective.
Economic and
Environmental Considerations
There is growing concern about the
environmental impact of inhaled
anesthetics due to their contribution to
greenhouse gas emissions. Efforts are
being made to develop systems for
reclaiming and reusing these agents
 during surgeries to minimize their
environmental footprint.
3.Muscle relaxant
Muscle relaxants are prescription
medications that help alleviate muscle-
related symptoms such as spasms,
spasticity, and musculoskeletal pain.
They primarily fall into two categories:
antispastics and antispasmodics.
Antispastics target conditions like
spasticity, while antispasmodics focus on
reducing muscle spasms.
Types of Muscle Relaxants
1.Antispastics: These
medications act directly on the spinal cord
or skeletal muscles to reduce tightness
and involuntary contractions. Common
examples include baclofen and
dantrolene.
2.Antispasmodics: These work by
affecting the central nervous system to
inhibit signals that cause muscle
spasms. Examples include
cyclobenzaprine and carisoprodol.
Usage and Administration
Muscle relaxants are typically prescribed
for short-term use due to their potential
side effects, including sedation,
dizziness, and the risk of dependence or
addiction with certain types like
diazepam and carisoprodol. They can be
administered in various forms such as
tablets, capsules, or injections.
Side Effects and Risks
Common side effects include drowsiness,
fatigue, dizziness, and confusion. More
serious risks involve potential overdose
or dangerous interactions with alcohol. It
is crucial for patients to discuss their
medical history with healthcare
providers before starting these
medications.
4.Adjuvant
An adjuvant drug is a substance that
enhances the efficacy or potency of
other medications. In pharmacology,
adjuvants are often used in various
therapeutic contexts, including cancer
treatment, pain management, and
vaccine formulation.
Types of Adjuvant Drugs
 1.Adjuvant Therapy in Cancer
Management:
Adjuvant therapy refers to additional
treatment given after the primary
treatment to eliminate any remaining
cancer cells. This approach is commonly
utilized in cancers such as breast, colon,
and lung cancer. The goal is to reduce
the risk of recurrence by targeting
microscopic cancer cells that may not be
detectable through imaging tests.
2.Analgesic Adjuvants in Pain
Management:
These are drugs that are not primarily
designed for pain relief but have
analgesic properties when used
alongside traditional pain medications
like opioids. Common examples include
antidepressants and anticonvulsants,
which can enhance pain relief and
address concurrent symptoms.
3.Immunologic Adjuvants
in Vaccines:
In the context of vaccines, adjuvants are
substances added to enhance the
immune response to the vaccine’s active
ingredient. They help improve the
effectiveness of vaccines by stimulating
a stronger immune reaction, thereby
providing better protection against
diseases.
Mechanism of Action
Adjuvants work through various
mechanisms depending on their
application:In cancer therapy, they may
target residual cancer cells.In pain
management, they can modulate
neurotransmitter systems or reduce
inflammation.In immunology, they can
activate immune pathways to boost
antibody production.
Clinical Applications
Healthcare providers consider several
factors when recommending adjuvant
therapies, including the type and stage
of cancer or condition being treated. For
instance:In breast cancer treatment,
radiation therapy may be recommended
post-surgery.In colorectal cancer cases,
chemotherapy might be suggested for
patients with advanced stages.For
chronic pain conditions, combining
opioids with adjuvant analgesics can
lead to improved outcomes while
minimizing opioid use.
 5.Reversal agent
Flumazenil
Flumazenil is a short-acting
benzodiazepine antagonist used to
reverse sedation caused by
benzodiazepines. It is administered
intravenously at a dose of 0.01 mg/kg,
with a maximum dose of 0.2 mg. If the
desired level of consciousness is not
achieved within 45 seconds, a repeat
dose of 0.005–0.01 mg/kg can be given.
The induction time for flumazenil is
between 1 to 3 minutes, with peak
effects occurring at 6 to 10 minutes.
However, its duration of effect is usually
less than 60 minutes, which may
necessitate additional doses due to the
possibility of re-sedation as the effects of
the benzodiazepine may last longer than
those of flumazenil.
Naloxone
Naloxone is an opioid antagonist that
reverses opioid-induced sedation by
competing with opioids at receptor sites.
It can be administered intravenously at a
dose of 0.01 mg/kg over 30 seconds and
may be repeated every 2–3 minutes as
needed based on patient response. The
onset of action occurs within 2 minutes,
but its duration typically lasts between
20 to 60 minutes, which may also lead to
re-sedation if the opioid’s effects persist
longer than naloxone’s.
Nalmefene
Nalmefene is another opioid reversal
agent available by prescription that
functions similarly to naloxone but has a
longer half-life and may cause more
severe withdrawal symptoms in patients
dependent on opioids.
Idarucizumab
Idarucizumab is specifically designed for
reversing dabigatran, a direct thrombin
inhibitor. It binds irreversibly to
dabigatran and provides immediate
reversal in cases of uncontrolled
bleeding or urgent surgical procedures.
Andexanet Alfa
Andexanet alfa serves as a reversal
agent for factor Xa inhibitors such as
apixaban and rivaroxaban. It acts by
binding these anticoagulants and
restoring normal coagulation activity.
2.1 Different categories of anticancer
drugs
 Introduction...
Anticancer drugs are pharmacological
agents that are effective in treating
malignant diseases,
commonly referred to as cancer. The
classification of these drugs is based on
their
mechanisms of action and includes
several
major categories: alkylating agents,
antimetabolites, natural products, and
hormones. Additionally, there are other
drugs
that do not fit neatly into these
categories but
still exhibit anticancer activity
.

⇛ 2.1.1Types of anti
cancer drug
1.Cytotoxic theraphy
Mechanism of Action (MOA)
The mechanism of action for cytotoxic
therapy
varies depending on the specific drug or
treatment used. However, the general
principle
involves targeting the cell cycle and
disrupting
processes necessary for cell division and
proliferation. Here are some common
mechanisms:
1.Alkylating Agents: These drugs
damage DNA by adding alkyl groups to
DNA
bases, leading to cross-linking and
preventing
DNA replication.
2.Antimetabolites: These mimic
natural
substances within the cell, interfering
with
DNA synthesis and function by inhibiting
enzymes involved in nucleotide
production.
3.Topoisomerase Inhibitors: These
prevent the action of topoisomerase
enzymes
that are crucial for DNA unwinding
during
replication, leading to DNA breaks.
4.Mitotic Inhibitors: These disrupt
microtubule formation during mitosis,
preventing proper cell division.
5.Antitumor Antibiotics: These bind to
DNA and interfere with RNA synthesis,
ultimately
leading to cell death.
Each class has its own specific targets
and
methods for inducing cytotoxicity in
cancer
cells.
Side EffectsWhile cytotoxic
therapies are effective against
cancer cells, they also affect normal fast-
growing cells in the body, leading to a
range
of side effects. Common side effects
include:


Fatigue: A common experience due to

the
overall impact on energy levels.


Hair Loss: Resulting from damage to

hair
follicle cells.


Nausea and Vomiting: Often due to

irritation of the gastrointestinal tract
lining.


Anemia: Caused by reduced red blood

cell
production in bone marrow.


Increased Risk of Infection: Due to

neutropenia (low white blood cell count).

Mouth Sores: Resulting from damage
to
mucosal cells in the oral cavity.


Changes in Appetite or Weight Loss:

Often
linked with nausea or changes in
metabolism.
The severity and occurrence of these
side
effects can vary widely among
individuals
based on factors such as overall health,
specific drugs used, and treatment
duration.Therapeutic Use
Cytotoxic therapy is primarily utilized in
treating various types of cancer. Its
therapeutic
applications include:
1.Curative Treatment: In some cases,
cytotoxic agents can eliminate cancer
completely.
2.Adjuvant Therapy: Used after
surgery or
radiation therapy to eliminate residual
disease
and reduce recurrence risk.
3.Neoadjuvant Therapy: Administered
before surgery to shrink tumors for
easier
removal.
4.Palliative Care: To relieve symptoms
associated with advanced cancer when
curative
options are not available.
Cytotoxic therapies may be used alone
or in
combination with other treatments such
as
immunotherapy or targeted therapies
depending on the type and stage of
cancer
being treated.
⇛ Alkalytic agent
Mechanism of Action (MOA)
Alkylating agents are a class of
chemotherapy
drugs that work by adding an alkyl group
to
the guanine base in DNA. This process
interferes with the normal linking of the
DNA
strands in the double helix structure,
leading
to DNA strand breakage. The disruption
in
DNA integrity prevents cancer cells from
successfully replicating and dividing,
ultimately
resulting in cell death. Alkylating agents
are
effective throughout all phases of the
cell cycle,
making them versatile for treating
various
types of cancers.
Side Effects
While alkylating agents are effective
against
cancer cells, they also affect normal cells
that
divide frequently. This can lead to
several side
effects, including:
1.Gastrointestinal Toxicity: Nausea,
vomiting, and diarrhea are common due
to
damage to the rapidly dividing cells in
the
gastrointestinal tract.
2.Bone Marrow Suppression: This can
result in decreased production of blood
cells,leading to anemia (low red blood
cell count),
increased risk of infections (low white
blood cell
count), and bleeding complications (low
platelet
count).
3.Reproductive Toxicity: Alkylating
agents can affect reproductive organs,
potentially leading to infertility or other
reproductive health issues.
4.Secondary Cancers: Long-term use
may increase the risk of developing
secondary
malignancies due to their mutagenic
potential.
Therapeutic Use
Alkylating agents have been used since
the
early days of chemotherapy and remain
important in cancer treatment today.
They are
particularly effective for treating:


Leukemia: Especially acute forms due

to
their ability to target rapidly dividing
cells.


Solid Tumors: Such as those found in

breast, lung, ovarian, and prostate
cancers.


Lymphomas and Myelomas: Including

Hodgkin’s disease.
Sarcomas: Various types that arise from
connective tissues.
Their broad applicability across different
cancer types makes them a staple in
oncological therapies.
In summary, alkylating agents play a
critical
role in cancer treatment through their
mechanism of action that disrupts DNA
function while also presenting significant
side
effects due to their impact on normal
dividing
cells.
⇛ Antimetabolite drug
(MOA) Antimetabolites function
as “cytotoxic”
agents, meaning they kill cells by
disrupting
their ability to replicate. They act as
decoys
that resemble the correct metabolites
required
for DNA and RNA synthesis. When cancer
cells
attempt to use these antimetabolites,
they end
up sabotaging their own genetic code,
which
prevents them from making copies of
themselves. This is particularly effective
againstrapidly dividing cancer cells, as
antimetabolites
target these cells during their division
phase.
There are three main types of
antimetabolites:
1.Purine antagonists - These mimic
purines, which are essential components
of DNA.
2.Pyrimidine antagonists - These
mimic pyrimidines, another set of
building
blocks for DNA.
3.Folic acid antagonists - These
inhibit
the utilization of folic acid in DNA
synthesis.
Therapeutic Use
Antimetabolites are
commonly used to treat various types of
cancers, including:


Leukemias


Breast cancer


Ovarian cancer


Colorectal cancer


Lung cancer
They can be administered in several
forms:
orally as tablets or liquids, through
intravenous(IV) injections, or topically as
creams for skin
cancers.
Side Effects While
antimetabolites
can be effective in killing cancer cells
and
preventing tumor growth, they also
come with
a range of potential side effects due to
their
impact on healthy fast-dividing cells.
Common
side effects include:


Nausea and vomiting



Loss of appetite


Fatigue and weakness



Mouth sores or inflammation



Hair loss


Skin rashes or dryness



Diarrhea or constipation


Changes in vision or light sensitivity



Lower white blood cell counts, increasing

infection risk
The specific side effects can vary
depending on
the particular antimetabolite being
used.In summary, antimetabolite
drugs work by
mimicking essential molecules
needed for
DNA and RNA synthesis in rapidly
dividing
cancer cells, thereby preventing
replication
and leading to cell death. They are
utilized in
treating various cancers but may cause
significant side effects due to their
action on
both malignant and healthy fast-dividing
cells.
⇛ Antitumor antibiotics
Mechanism of Action (MOA)
The mechanism of action for antitumor
antibiotics involves their interaction with
DNA
in cancer cells. These drugs can bind to
DNA
and interfere with its replication and
transcription processes. This disruption
leads
to cell death or inhibits the ability of
cancer
cells to multiply. Antitumor antibiotics
can be
categorized into two main groups based
on
their structure and mechanism:
1.Anthracyclines: This group includes
drugs such as daunorubicin, doxorubicin,
epirubicin, idarubicin, mitoxantrone, and
valrubicin. Anthracyclines primarily work
by
intercalating into DNA strands,
disrupting thefunction of topoisomerase
II, an enzyme
critical for DNA replication. This
interference
prevents cancer cells from effectively
copying
their DNA before cell division.
2.Miscellaneous Antitumor
Antibiotics:
This category includes bleomycin,
dactinomycin, and mitomycin C. For
example
3.Bleomycin binds to DNA and
generates free radicals that cause
oxidative
damage.
4.Dactinomycin binds to DNA and
inhibits mRNA synthesis, which is
essential for
protein production.
5.Mitomycin C damages DNA directly
by cross-linking it.
Side Effects
Antitumor antibiotics are associated with
a
range of side effects due to their impact
on
both cancerous and healthy cells.
Common
side effects include:


Fever and chills



Fatigue
General malaise


Rash


Hair loss


Loss of appetite


Nausea or vomiting


Diarrhea


Mouth and throat sores



Anemia


Easy bruising or bleeding


Skin and nail discoloration


Increased risk of infections



Fertility issues
Specific risks are also associated with
certain
types of antitumor antibiotics:


Anthracyclines can lead to heart

damage,
especially at high doses or in patients
with
pre-existing heart conditions.


Bleomycin is known for its potential to

cause lung damage or fibrosis.Patients
receiving these treatments are
typically monitored for signs of these
serious
side effects through various tests.
Therapeutic Use
Antitumor antibiotics are utilized in the
treatment of numerous cancers
depending on
the specific drug’s efficacy against
particular
types. Here’s how some antitumor
antibiotics
are used therapeutically
1.Anthracyclines
Doxorubicin: Used for breast cancer,
acute lymphocytic leukemia (ALL), acute
myeloid
leukemia (AML), lymphoma (both
Hodgkin’s and
non-Hodgkin’s), among others.
Daunorubicin: Primarily used for ALL
and AML.
Epirubicin: Mainly used in breast
cancer treatment.


Idarubicin: Used specifically for AML.



Mitoxantrone: Effective against acute

non-lymphocytic leukemia (ANLL) and
prostate cancer.
Valrubicin: Administered specifically
for bladder cancer.
2.Miscellaneous Antitumor
Antibiotics
Bleomycin: Treats lymphoma
(Hodgkin’s and non-Hodgkin’s),
squamous cell
carcinomas (head/neck/cervix/vulva),
metastatic
testicular cancer.
Dactinomycin: Utilized in childhood soft
tissue sarcoma, Ewing’s sarcoma,
testicular
cancer, Wilms’ tumor.


Mitomycin C: Employed in various

cancers including bladder cancer.
The choice of which antitumor antibiotic
to use
depends on factors such as the type of
cancer
being treated, its stage, previous
treatments
received by the patient, overall health
status,
age, and personal preferences.
⇛ Mitotic inhibitor
Mechanism of Action (MOA)
The mechanism of action for mitotic
inhibitors
involves their ability to bind to tubulin,
aprotein that polymerizes to form
microtubules.
Microtubules play a crucial role in the
formation of the mitotic spindle, which is
essential for separating chromosomes
during
cell division. There are two main classes
of
mitotic inhibitors based on their action:
1.Tubulin Depolymerization
Inhibitors:
These drugs prevent the assembly of
microtubules. For example, vinca
alkaloids like
vincristine and vinblastine bind to
tubulin
dimers and inhibit their polymerization
into
microtubules, leading to reduced
microtubule
mass and disruption of the mitotic
spindle
2.Tubulin Polymerization Inhibitors:
These agents stabilize microtubules and
prevent their disassembly. Paclitaxel
(Taxol) is a
well-known example that binds to the β-
tubulin subunit and promotes
microtubule
stabilization, preventing normal
depolymerization processes that would
allow
for proper chromosome segregation.
By disrupting these processes, mitotic
inhibitors effectively halt cell division at
variousstages of the cell cycle,
particularly during
metaphase and anaphase.
Side Effects
While effective in treating cancer,
mitotic
inhibitors can also cause significant side
effects
due to their impact on normal rapidly
dividing
cells in the body. Common side effects
include:


Chemotherapy-Induced Peripheral
Neuropathy: Damage to peripheral
nerves can
lead to pain, tingling sensations, or
numbness.


Bone Marrow Suppression: This can

result
in decreased production of blood cells
leading
to anemia, increased risk of infection
(due to
low white blood cell counts), and
bleeding
issues (due to low platelet counts).


Gastrointestinal Disturbances:
Nausea,
vomiting, diarrhea, or constipation may
occur.


Hair Loss: Alopecia is common with

many
chemotherapeutic agents.


Fatigue: General tiredness due to both

direct effects on cells and secondary
effects
from anemia or other factors.These side
effects vary depending on the
specific drug used and individual patient
responses.
Therapeutical Use
Mitotic inhibitors are primarily utilized in
oncology for treating various types of
cancers
due to their effectiveness against rapidly
dividing tumor cells. Some therapeutic
uses
include:


Paclitaxel (Taxol): Used for breast

cancer,
ovarian cancer, lung cancer, and
Kaposi’s
sarcoma.


Vincristine and Vinblastine:

Employed in
treating leukemias (such as acute
lymphoblastic leukemia), lymphomas
(including Hodgkin’s lymphoma),
testicular
cancer, and breast cancer.


Colchicine: While not typically used for

cancer treatment in humans, it is
effective for
gout management due to its ability to
inhibit
inflammatory responses by disrupting
microtubule dynamics.In addition to
oncology applications, some
mitotic inhibitors have roles in
cytogenetics
where they are used to halt cell division
at
specific stages for chromosomal
analysis.
⇛ Hormonal therapy
Mechanism of Action (MOA)
Hormone therapy works by targeting
specific
hormones that certain cancers depend
on for
growth. The mechanism can vary
depending
on the type of hormone therapy used
1.Stopping Hormone Production:
Some
therapies inhibit the body’s ability to
produce
hormones. For example, Luteinizing
hormone
releasing hormone (LHRH) agonists
reduce
testosterone production in men and
estrogen
production in women.
2.Blocking Hormone Receptors:
Other
therapies block the receptors that
hormones
bind to on cancer cells, preventing them
from
receiving the signals they need to grow.
Selective estrogen receptor modulators
(SERMs), such as tamoxifen, are
examples that
block estrogen receptors in breast
cancer cells.3.Altering Hormones:
Certain treatments
modify hormones so they do not function
as
intended. For instance, aromatase
inhibitors
prevent the conversion of androgens
into
estrogens in postmenopausal women.
4.Surgical Removal of Hormone-
Producing Organs: In some cases,
surgery may
be performed to remove organs that
produce
hormones, such as ovaries or testicles.
Side Effects
The side effects of hormone therapy can
vary
widely based on the specific treatment
and
individual patient factors. Common side
effects
include:


Fatigue: A general feeling of tiredness

that
can interfere with daily activities.


Hot Flashes: Sudden feelings of warmth

often accompanied by sweating.


Weight Gain: Increased appetite and

fluid
retention may lead to weight gain.


Decreased Sexual Desire: Many

patients
report a reduced interest in sexual
activity.
Erectile Dysfunction (ED): Men
undergoing
hormone therapy for prostate cancer
may
experience difficulties achieving or
maintaining
an erection.


Bone Loss/Osteoporosis: Long-term

use
can lead to decreased bone density and
increased fracture risk.


Mood Changes: Patients may

experience
mood swings or depression.
Other potential side effects include
nausea,
joint pain, vaginal dryness (in women),
and an
increased risk of blood clots.
Therapeutic Use;
Hormone
therapy is primarily used for treating
cancers
that are hormone-sensitive:
1.Breast Cancer: Hormone therapies
like
SERMs (e.g., tamoxifen) and aromatase
inhibitors are commonly used for
estrogen
receptor-positive breast cancer.
2.Prostate Cancer: Anti-androgens and
LHRH agonists are utilized to
lowertestosterone levels or block its
action in
prostate cancer treatment.
3.Endometrial Cancer: Progestins and
other hormonal agents can be effective
in
treating certain types of endometrial
cancer.
4.Adrenal Cancer: Adrenolytics like
mitotane are used to manage adrenal
tumors
5.Fertility Preservation or
Management in Transgender
Individuals:
Hormonal treatments may also be part
of care
for transgender individuals undergoing
gender
transition who have a diagnosis of
cancer
3. therapeutic uses of steroid
hormones
Introduction…
Steroid hormones, particularly
corticosteroids, are widely used in
medical practice due to their potent anti-
inflammatory and immunosuppressive
properties. They mimic the effects of
hormones produced naturally by the
adrenal glands, such as cortisol. Here’s a
detailed overview of their therapeutic
uses:
1. Treatment of Inflammatory
Conditions
Corticosteroids are primarily used to
manage various inflammatory
conditions. They help reduce
inflammation and alleviate symptoms
associated with diseases like rheumatoid
arthritis, lupus, and vasculitis. By
decreasing the production of
inflammatory chemicals in the body,
steroids can significantly relieve pain,
swelling, and stiffness.
2. Management of Autoimmune
Disorders
In autoimmune disorders, where the
immune system mistakenly attacks
healthy tissues, corticosteroids play a
crucial role. Conditions such as multiple
sclerosis and systemic lupus
erythematosus often require steroid
therapy to suppress the overactive
immune response and prevent further
tissue damage.
3. Control of Allergic Reactions
Steroids are effective in treating severe
allergic reactions or anaphylaxis. They
help reduce swelling and inflammation in
response to allergens, providing relief
from symptoms such as hives, itching,
and difficulty breathing.
4. Respiratory Conditions
In respiratory diseases like asthma and
chronic obstructive pulmonary disease
(COPD), corticosteroids are used to
decrease airway inflammation. Inhaled
corticosteroids are commonly prescribed
for long-term management of asthma to
improve lung function and reduce
exacerbations.
5.Dermatologcal application
Topical corticosteroids are frequently
used to treat skin conditions such as
eczema, psoriasis, and dermatitis. These
creams or ointments help reduce
redness, itching, and inflammation
directly at the site of application.
 6. Endocrine Disorders
Corticosteroids can also be used in cases
of adrenal insufficiency (Addison’s
disease) where the body does not
produce enough natural steroids.
Replacement therapy with synthetic
corticosteroids helps maintain normal
physiological functions.
7.Cancer treatment
In oncology, steroids may be utilized as
part of chemotherapy regimens to
mitigate side effects like nausea or to
enhance the effectiveness of certain
treatments by reducing inflammation
around tumors.
8. Organ Transplantation
After organ transplants, corticosteroids
are administered to prevent rejection by
suppressing the immune system’s
response against the transplanted organ.
9. Hematological Disorders
Corticosteroids can be beneficial in
treating blood disorders such as
thrombocytopenia (low platelet count) or
certain types of anemia by modulating
immune responses that affect blood cell
production.
In summary, steroid hormones have
diverse therapeutic applications across
various medical fields due to their ability
to modulate inflammation and immune
responses effectively.

4.Explain the mechanism of

action of hormonal
contraceptives and list the
different?
Mechanism of Action of
Hormonal Contraceptives;Hormonal
contraceptives are methods of birth
control that utilize hormones to prevent
pregnancy. They primarily work through
three main mechanisms:
1.Inhibition of Ovulation:
The primary action of hormonal
contraceptives is the suppression of
ovulation. This is achieved by providing
exogenous hormones (estrogen and
progestin) that mimic the natural
hormones in the body. When these
hormones are present at sufficient
levels, they signal the hypothalamus and
pituitary gland to reduce the secretion of
gonadotropins (luteinizing hormone (LH)
and follicle-stimulating hormone (FSH)).
This inhibition prevents the ovarian
follicles from maturing and releasing an
egg, thereby preventing ovulation.
2.Thickening of Cervical
Mucus:
Hormonal contraceptives also lead to
changes in cervical mucus. Progestins
cause the cervical mucus to thicken,
making it more viscous and less
permeable to sperm. This thickened
mucus acts as a barrier, reducing sperm
motility and their ability to reach any
eggs that may have been released.
3.Alteration of Endometrial
Lining:
Hormonal contraceptives alter the
endometrial lining (the inner lining of the
uterus). The presence of progestins
leads to a thinner endometrium, which
makes it less suitable for implantation
should fertilization occur. If an egg were
to be fertilized, a poorly developed
endometrial lining would decrease the
likelihood of successful implantation.
Types of Hormonal
Contraceptives
Hormonal contraceptives can be
categorized into several types based on
their formulation and delivery method:
1.Combined Oral
Contraceptives (COCs):These pills
contain both estrogen and progestin.
They are taken daily for 21 days
followed by a week off or placebo pills
during which menstruation occurs.
2.Progestin-Only Pills
(POPs):Also known as “mini-pills,” these
contain only progestin without estrogen.
They must be taken at the same time
every day for maximum effectiveness.
3.Contraceptive Patches:
These transdermal patches release both
estrogen and progestin into the
bloodstream through the skin. They are
typically worn for a week at a time.
1.Vaginal Rings:A flexible
ring that is inserted into the vagina,
releasing both estrogen and progestin
over a period of three weeks, followed
by a week without the ring
2.Injectable
Contraceptives:
These involve administering progestin
via injection every three months (e.g.,
Depo-Provera).
3.Implants:
Subdermal implants release progestin
over an extended period (up to three
years), providing long-term
contraception.
1.Intrauterine Devices
(IUDs):Some IUDs release hormones
(progestins) locally within the uterus,
providing effective contraception for
several years while altering endometrial
conditions.
2.Emergency Contraceptive
Pills (ECPs):These can contain either
levonorgestrel or ulipristal acetate and
are used after unprotected intercourse
to prevent ovulation or alter endometrial
receptivity if taken within a specific
timeframe post-intercourse.
In summary, hormonal contraceptives
function mainly by inhibiting ovulation,
thickening cervical mucus, and altering
uterine lining conditions, with various
forms available depending on individual
needs and preferences.

5.Discuss the pharmacology of

antiprotozoal medications?
Pharmacology of Antiprotozoal
Medications
Antiprotozoal medications are a class of
drugs specifically designed to treat
infections caused by protozoa, which are
single-celled eukaryotic organisms.
These medications work through various
mechanisms to inhibit the growth or kill
the protozoan parasites responsible for
diseases such as malaria, giardiasis,
Chagas disease, and African
trypanosomiasis (sleeping sickness).
Mechanisms of Action
1.DNA Damage and Replication
Inhibition: Many antiprotozoal agents,
such as metronidazole, function by
damaging the DNA of protozoans. This
can occur through the formation of free
radicals that cause breaks in the DNA
strands or by inhibiting DNA replication
processes. By disrupting these vital
cellular functions, the medications
effectively limit the ability of the
protozoa to reproduce and spread.
2.Inhibition of Folic Acid
Synthesis: Some antiprotozoal drugs
inhibit folic acid synthesis within
protozoan cells. This is crucial because
folic acid is necessary for nucleic acid
synthesis and cell division. For instance,
trimethoprim-sulfamethoxazole targets
this pathway, leading to impaired growth
and replication of the parasites.
3.Energy Metabolism
Disruption: Certain antiprotozoal
agents affect energy metabolism in
protozoans. For example, suramin
interferes with glucose utilization in
trypanosomes, which is essential for
their energy production. By disrupting
these metabolic pathways, these drugs
render the parasites unable to sustain
their life processes.
 4.Binding to Cellular
Components: Some medications may
bind directly to components within
protozoan cells, affecting their function.
Pentamidine isethionate is believed to
bind to DNA within Pneumocystis carinii
(now known as Pneumocystis jirovecii),
thereby inhibiting its replication.
TypesofAntiprotozoalMedicatio
ns
1.Metronidazole: Commonly
used for treating infections like giardiasis
and bacterial vaginosis; it works
primarily by causing DNA damage.
2.Iodoquinol: Used for
amoebiasis; it inhibits several enzymes
critical for protozoan survival.
3.Nifurtimox: Effective against
Trypanosoma cruzi (Chagas disease) by
producing reactive oxygen species that
are toxic to the parasite.
4.Suramin: Used for African
trypanosomiasis; it disrupts glucose
metabolism in trypanosomes.
5.Chloroquine Phosphate:
Primarily used for malaria treatment; it
 interferes with heme detoxification in
Plasmodium species
6.Administration Routes
Antiprotozoal medications can be
administered through various routes
depending on the specific drug and
infection being treated:
Oral administration is common for many
agents like metronidazole and
chloroquine.
Intravenous administration may be
required for drugs like suramin due to
poor gastrointestinal absorption.
Side Effects
While effective against protozoan
infections, antiprotozoal medications can
have side effects including:
 Gastrointestinal issues such as nausea,
vomiting, diarrhea, and abdominal pain.
 Hematological effects like anemia or
leukopenia.
 Neurological symptoms including
dizziness or peripheral neuropathy.
 Rare but severe reactions such as kidney
damage or shock.
Patients receiving these medications
should be monitored closely for adverse
effects and educated about potential
interactions with other drugs or
substances like alcohol.
The pharmacology of antiprotozoal
medications highlights their diverse
mechanisms of action aimed at
combating various parasitic infections
while also necessitating careful
management due to potential side
effects.

REFFERENCE
1. Drug.com(https://www.drug.com
2. Pubmed(https://pubmed.ncbi.nlm.nih.gov
3. National institute of health(https://clinicaltrial.gov