Malaria disease and Anti-malarial drugs

Malaria:
- Estimated 300-500 million human infections per year throughout the world
- Transmitted to humans through the bite of female Anopheles mosquitoes
- The parasite Plasmodium spp cause infections in humans that is transmitted by the vector (mosquito).

Four major species are identified namely P falciparum, P vivax, P ovale, P malariae

Clinically Important Anti-Malarial Drugs, Prevention

and Treatment of Malaria:
The four most important and widely used drugs for the treatment of malaria:
1.Chloroquine and Hydroxychloroquine
2. Quinine
3. Primaquine
4. Antifolates

1. Chloroquine (4-Aminoquinololines) and hydroxychloroquine (HCQ)

Clinical Indication
- Chloroquine (CQ) is mostly effective against all four types of malaria (except chloroquine-resistant P
falciparum)
- Hydroxychloroquine is the analog of a chloroquine, a less toxic metabolite of CQ.
- Used in the treatment of acute malaria
- Malaria prophylaxis
- HCQ for rheumatoid arthritis or systemic lupus erythematosus

Mechanism of Action
- Chloroquine is effective during an intraerythrocytic stage of the parasite.
- The drug concentrates into the parasite-infected erythrocytes and enters the food vacuole of the
parasite by an ion-trapping mechanism.

Mechanism of action:
- intercalation with DNA, inhibition of heme polymerase
- interaction with Ca++-calmodulin mediated mechanism
- inhibit peptide formation and phospholipases leading to parasite death

Absorption, Metabolism, and Excretion

- Rapidly absorbed from the intestine
- approximately 50% bound to plasma proteins
- about 70% of a dose is excreted unchanged in the urine
- half live is 120 hours

Toxicity (side effects)

- mild headache, visual disturbances, gastrointestinal upsets & pruritus are observed during short term
therapy
- After prolonged therapy, ocular damage, retinopathy (bulls-eye macula), lichenoid skin eruption,
bleaching of hearing, etc. may be observed

Drug Interaction
- Chloroquine and quinine are antagonistic and should not be used in combination.

2. Quinine (4-aminoquinoline derivatives/ Quinoline derivative)

Clinical Indications
- Quinine is the main alkaloid of cinchona bark (tree).
- drug of choice in the treatment of an acute attack of falciparum malaria where the parasite is known
to be resistant to chloroquine.
- may be given intravenously and then orally when patients start to improve
- Doxycycline or clindamycin may be used as combination therapy with quinine.

Mechanism of action:
- the mechanism for anti-malarial activity remains unclear for quinine.

Absorption, Metabolism, and Excretion

- Quinine is almost completely absorbed in the upper part of the small intestine
- peaks after 1-3 hours of ingestion
- half live is approximately 10 hours
- metabolized in the liver (95%) to inactive hydroxy derivatives
- approximately 5% is excreted in urine as an unchanged drug

Toxicity (side effects)

- Quinine may cause Cinchonism (neural, retinal and auditory toxicity)
- Abdominal pain and diarrhea
- Rashes, fever, renal failure, hemolytic anemia, thrombocytopenia (too low platelet count in blood),
etc.

3. Primaquine/ Primaquine phosphate

Clinical Indication:
- used to eradicate hepatic form of P vivax or P malariea infections after standard chloroquine therapy.
- may be used prophylactically with chloroquine

Mechanism of action:
- inhibits the electron transport chain in mitochondria (structurally similar to coenzyme Q) of parasite

Absorption, Metabolism, and Excretion:

-Primaquine is rapidly absorbed from the gastrointestinal tract
- not bound to tissues
- rapidly metabolized and the metabolites may be pharmacologically active as the parent compound
- peaks after 4-6 hours after ingestion
- short half-life and almost completely eliminated from the body by 24 hours

Toxicity (side effects):

- Primaquine have shown to cause lethal hemolysis in individuals with glucose-6-phosphate
dehydrogenase deficiency
- higher dose or prolonged exposure can cause;
• gastrointestinal distress nausea
• nausea
• headache
• pruritus (itchy skin)
• leukopenia (low WBC- white blood cell)
4. Antifolates (Pyrimethamine)

- inhibits folate metabolism at all stages of parasite life cycles

- serves as a competitive inhibitor of the malarial dihydrofolate reductase

- limited use in malaria prophylaxis due to emergence of resistance

Frequently Asked Questions

What is the difference between analgesics and antipyretics?

An analgesic relieves pain, by either reducing an inflammation or by changing the method in
which your brain recognizes pain. An antipyretic, specifically reduces fevers by overriding the
prostaglandin induced increase in body temperature, reducing the amount of inflammatory
cytokines in the bloodstream.
What does "antipyretic" mean in medical terms?
Antipyretics are used to reduce or eliminate a fever. Some operate by the indirect means and
treat the root cause of the fever, such an an inflammatory response to a viral or bacterial
infection, others act directly on the symptoms of the inflammation, pain and or discomfort.

What does the word antipyretic mean in medical terms?

An antipyretic is a pharmaceutical agent or a non-pharmacological agent that reduces or
eliminates a fever, usually induced by some source of inflammation.

Naming a Drug
A marketed drug has three names: a chemical name, a generic
name, and a brand name. A chemical name is given when a new
chemical entity (NCE) is developed. The chemical name is a
scientific name based on the compound's chemical structure
(e.g., 6-thioguanine) and is almost never used to identify the drug
in a clinical or marketing situation. The generic name is granted
by the USAN Council and is commonly used to identify a drug
during its useful clinical lifetime. The company that patents the
drug creates the brand name (trademark). This name identifies
the drug during the 17 years that the company has exclusive
rights to make, sell, and use it under patent law.

The process for naming a marketable drug involves five steps:

NCE submission and patent application, generic naming, brand
naming, FDA review, and final approval.

Anthelmintics: Generic and Brand Names

Here is a table of commonly encountered anthelmintics, their generic names,
and brand names:
Antihelmintics
albendazole (Albenza)
ivermectin (Stromectol)
mebendazole (Vermox)
praziquantel (Biltricide)
pyrantel (Antiminth)
Disease Spotlight: Helminthic infections
These are infections in the GI tract or other tissues due to worm
infestations. It affects about 1 billion people which make it the most common
of all diseases.
Infestations are very common in tropical areas. Travelers can contract a
helminthic infection and bring it home, where the worms can infect other
individuals.
Most common infectious helminths are nematodes (roundworms) and
platyhelminthes (flatworms) which invade the intestines and the tissues.
Therapeutic Action
The desired and beneficial action of anthelmintics is:
They act on metabolic pathways present in the invading worm but are
absent or significantly different in human host.
Indications
Anthelmintics are indicated for the following medical conditions:
Albendazole for the treatment of active lesions caused by pork tapeworm
and cystic disease of the liver, lungs, and peritoneum caused by dog
tapeworm.
Ivermectin is used for the treatment of threadworm disease or
strongyloidiasis and onchocerciasis or river blindness.
Mebendazole is for the treatment of diseases caused by pinworms,
roundworms, whipworms, and hookworms.
Praziquantel is for treatment of a wide number of schistosomes or flukes.
Pyrantel is for treatment caused by pinworms and roundworms.
Here are some important aspects to remember for indication anthelmintics
in different age groups:
Children
Culture of the suspected worm is important before beginning any drug
therapy.
Albendazole, ivermectin, and praziquantel are more toxic so they are
avoided in children. Instead, a chewable preparation of mebendazole is
usually given.
Children may develop serious GI effects during therapy so nurse’s focus
must be on nutritional status and hydration.
Adults
This age group might be repulsed by the idea that they have a worm
infestation, and they may be reluctant to discuss the needed lifestyle
adjustments and treatment plans.
Pregnant and nursing women should not use these drugs unless the
benefits clearly outweigh the risks. Potential risks must be communicated to
the patients.
Older adults
Older patients are more susceptible to GI and CNS adverse effects of
Anthelmintics therapy particularly those with hepatic and renal dysfunctions.
Pharmacokinetics
Here are the characteristic interactions of anthelmintics and the body in
terms of absorption, distribution, metabolism, and excretion:
Route Onset Peak Duration
Oral Slow 2-4 h N/A
T1/2: 2.5-9 h
Metabolism: liver
Excretion: colon (feces)
Contraindications and Cautions
The following are contraindications and cautions for the use of anthelmintics:
Known allergy to the drug. Prevent hypersensitivity reactions.
Lactation. Drug can enter breast milk.
Renal and hepatic disease. Interfere with drug metabolism and
excretion.
Severe diarrhea and malnourishment. Can alter effects of drug on
the intestine and any preexisting helminths.
Pyrantel has not been established as safe for use in children younger than
2 years.
Adverse Effects
Use of anthelmintics may result to these adverse effects:
GI: abdominal discomfort, diarrhea, pain
CNS: headache, dizziness,
Immunologic: fever, shaking, chills, malaise, rash, pruritus, loss of hair
Albendazole is associated with severe bone marrow depression and renal
failure.
Interactions
The following are drug-drug interactions involved in the use of anthelmintics:
Dexamethasone, praziquantel, cimetidine. Increased toxic effects of
albendazole
Nursing Considerations
Here are important nursing considerations when administering anthelmintics:
Nursing Assessment

These are the important things the nurse should include in

conducting assessment, history taking, and examination:
Assess for the mentioned cautions and contraindications (e.g. known
allergies, hepatorenal dysfunction, pregnancy and lactation, etc.) to prevent
any untoward complications.
Perform a thorough physical assessment (other medications taken, reflexes
and muscle strength, skin color, temperature, texture, etc.) to establish
baseline data before drug therapy begins, to determine effectiveness of
therapy, and to evaluate for occurrence of any adverse effects associated
with drug therapy.
Assess the patient’s liver function, including liver function tests to
determine appropriateness of therapy and to monitor for toxicity.
Obtain a culture of stool for ova and parasites to determine the infecting
worm and establish appropriate treatment.
Assess the abdomen to evaluate for any changes from baseline related to
the infection, identify possible adverse effects, and monitor for improvement.
Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of
these drugs for therapy:
Acute pain related to GI, CNS, and skin effects of the drug
Imbalanced nutrition: less than body requirements related to GI effects of
the drug

Anticholinergic drugs: What to know

• What are they?
• How they work
 • Uses
• List
• Side effects
• Interactions
• Summary
Anticholinergic drugs can treat a variety of conditions, including chronic obstructive pulmonary
disease (COPD), bladder conditions, and gastrointestinal disorders, among others.
Many typesTrusted Source of drugs produce anticholinergic effects. They all work by blocking the
action of acetylcholine, a type of neurotransmitter. Neurotransmitters are chemical messengers in the
brain. Blocking this neurotransmitter inhibits involuntary muscle movements and various bodily
functions.
Only a doctor can determine which anticholinergics are right for a person and how long the treatment
should last. The inappropriate use of anticholinergics can have severe adverse effects.
In this article, learn more about anticholinergic drugs, their uses, and possible side effects.

What is an anticholinergic?
Anticholinergics are a type of medication that blocks the action of a neurotransmitter called
acetylcholine. Acetylcholine transfers signals between cells that affect specific bodily functions.
The medication blocks acetylcholine from causing involuntary muscle movements in the lungs,
gastrointestinal tract, urinary tract, and other areas of the body.
As anticholinergics can affect a variety of functions, including digestion, urination, salivation, and
movement, they can help treat many conditions.

How do anticholinergics work?

Anticholinergic drugs work by blocking the activity of acetylcholine, a neurotransmitter, in the
cholinergic system. The cholinergic system plays a role in:
• movement
• the emotions
• thinking
The cholinergic system has two typesTrusted Source of receptors: muscarinic and nicotinic. Muscarinic
receptors function in the peripheral and central nervous systems and are present in various organs
throughout the body. Nicotinic receptors function in the central nervous system and at the
neuromuscular junction.
Anticholinergics block activity at both these types of receptors.
Uses
Anticholinergics can help treat various health conditions, includingTrusted Source:
• respiratory disorders, such as COPD
• overactive bladder and incontinence
• asthma
• symptoms of Parkinson’s disease, such as tremor
• cardiovascular disease
• gastrointestinal symptoms, such as vomiting
• allergies
• depression
Doctors may also prescribe anticholinergics such as orphenadrine as muscle relaxants. These drugs can
be useful during surgery to block neuromuscular reactions and stop saliva production.
Flavoxate and oxybutynin are antispasmodic agents, which means they can help prevent vomiting.
Clindinium, an anticholinergic drug that also contains chlordiazepoxide, is another example.
Some people use anticholinergics off-label for excessive sweating.

List of anticholinergics
Different types of anticholinergic drugs can treat different conditions or symptoms. These medications
are only available with a doctor’s prescription.
Anticholinergics include:
• atropine
• benztropine
• glycopyrrolate
• scopolamine
• trihexyphenidyl
• diphenhydramine
• clinidium
• flavoxate
• oxybutynin
• orphenadrine

Side effects
Anticholinergics are usually safe to use if a doctor prescribes them, but side effects can occur.
The risk of adverse effects will depend on the individual’s medical history, the dosage, and the type of
anticholinergics they take. Age may also be a factor.
Possible side effects include:
 • hyperthermia
• lack of sweating
• rapid or irregular heartbeat
• flushing
• urinary retention
• blurred vision
• glaucoma
• vision loss
• dilated pupils
• reduced muscle contraction
• headache
• problems with thinking and memory
• agitation
• behavioral changes
• anxiety
• insomnia
• delirium
• hallucinations
Some researchTrusted Source has linked the long-term use of anticholinergics in older people to an
increased risk of dementia. Before prescribing these drugs, a doctor should consider a person’s age,
health conditions, and other medications.
It is essential to remain hydrated when taking anticholinergics because they decrease sweating, which
may increase the risk of overheating.
Taking too many anticholinergics can result in anticholinergic toxicityTrusted Source, which may cause
a person to experience the side effects above to a more severe degree. If anyone notices these signs in
themselves or another person, they should seek emergency medical attention.

Interactions and contraindications

Doctors need to take careTrusted Source when prescribing anticholinergics, especially for older people
and those at risk of dementia.
Older people are more at risk because their blood-brain barrier is more permeable, which means the
active ingredients can pass more easily into the brain.
Taking too much of an anticholinergic or using more than one anticholinergic drug can also lead to
adverse effects.
Conditions that can worsen with the use of anticholinergics include:
• dementia
• glaucoma
• hyperthyroidism
• rapid or irregular heartbeat
 • enlarged prostate
• depression
• schizophrenia

Summary
Anticholinergics are medications that block the action of acetylcholine, a type of neurotransmitter. As a
result, they stop involuntary muscle movements and various bodily functions.
Anticholinergic drugs can help treat a range of conditions, including COPD, an overactive bladder,
gastrointestinal disorders, and symptoms of Parkinson’s disease.
Anticholinergics are only available via prescription, so it is best to speak with a doctor about which
type can help treat specific conditions. A doctor can also explain the risks and side effects.

What to know about drug interactions

• Types
• Other factors
• Reading drug labels
• Contacting a doctor
• Summary
A drug interaction happens when a substance affects how a drug behaves in the body. Some substances
that can cause interactions include other drugs, supplements, food, and alcohol.
Drug interactions can make a drug less effective. In some cases, they can make a drug more potent,
which can be dangerous.
The symptomsTrusted Source of drug interactions vary greatly and range from mild to life threatening.
Some common warning signs include feeling sick after taking a medication, not getting the usual
results from a medication, or feeling either very tired or very energetic after taking a medication.
Drug interactions do not only occur between prescription drugs. Over-the-counter drugs, food,
supplements, and alcohol can all change the way the body metabolizes (breaks down) medication.
Read more to learn about different types of drug interactions, risk factors, and how to help prevent
interactions by thoroughly reading drug labels.

Types of drug interactions

There are several types of drug interactions.

Drugs
Drug-drug interactions occur when one drug interacts with another.
Certain drugs are more prone to interactions than others. For example, warfarinTrusted Source is an
anticoagulant used to help prevent blood clots. It interacts with many other medications.
This is because a group of enzymes (called CYP450 enzymes) change the way the body metabolizes
warfarin. Drugs that inhibit these enzymes can increase the effects of warfarin, increasing the risk of
dangerous bleeding. Drugs that induce the enzymes reduce warfarin’s effectiveness, raising the risk of
blood clots.
These potentially dangerous health outcomes show how important it is to discuss new medications with

a doctor or pharmacist. ics and Disinfectants

Disinfectants and Antiseptics

What is Disinfectant?
A disinfectant can be defined as an antimicrobial agent that can be applied on the
surface of some objects in order to destroy the microorganisms residing on it.

What is an Antiseptic?
Antiseptics can be defined as antimicrobial agents which can be applied on the
body of living organisms to inhibit the action of microbes. They are not injected
into the body like the antibiotics, rather they are applied on the surface of the skin
to heal the living tissues in case of wounds and cuts.

Dettol is the most commonly used antiseptic. It is a mixture of chloroxylenol and

terpineol. Iodoform is also used as an antiseptic for wounds.

How does it destroy the micro-organisms?

The simple answer to this is – antimicrobial agents.

A disinfectant is an antimicrobial agent. It is not necessary that a disinfectant will

kill all the microorganisms. It is not as effective as sterilization. The process of
sterilization kills all types of living forms but a disinfectant kills only certain types
of microbes. It is generally applied to a floor or a drainage system. Most of the
popularly used cleaning products used in homes and offices are nothing but
disinfectants.
Types of Disinfectants
Some common types of disinfectants include:

1.Air disinfectants: It is defined as the chemical substances which are used to kill the
microorganisms that are suspended in the air. It can also be called as a disinfectant
spray.
2.Alcohol: It is seen that alcohols are used as disinfectants. Ethanol is the most
common example in this case. Some other examples of disinfectants are, chlorine
when it is in the concentration of 0.2 to 0.4 in aqueous solution and sulphur dioxide,
which acts as a disinfectant in small concentrations.

Types of Antiseptics
Some antiseptics are germicidal in nature, implying that they have the ability to
completely destroy microbes. These types of antiseptics are referred to as
bacteriocidal antiseptics. Other antiseptics only inhibit the growth of microbes (or
prevent the growth of microbes altogether). Such substances are commonly
referred to as bacteriostatic antiseptics.

The Difference between Disinfectants and Antiseptics

Disinfectants and antiseptics are both used for killing the microbes but still, there
is a difference between them.

•An antiseptic is used for killing the microbes on the living tissues whereas a
disinfectant is applied on a non-living object.
•Secondly, the concentration of both differ. We can use the same chemical as a
disinfectant and an antiseptic by varying its concentration.
•For example, phenol can be used as an antiseptic if its concentration is 0.2 % but to
use it as a disinfectant the concentration should be 1%.
•We can broadly conclude that the cleaning products contain disinfectants and the
healing products (for curing the living tissues) contain antiseptics.
•Both are similar in nature but vary in their concentration. Lysol is a disinfectant
whereas Dettol is an antiseptic.
 ANTIVIRALS

Introduction
Antiviral drugs are prescription medicines (tablets, liquids, an inhaled

powder, or an intravenous solution) that fight against viruses in the body. Key

Points about antiviral drugs:

•Able to enter the cells infected with a virus

•Interfere with viral nucleic acid synthesis and/or regulation

•Some agents interfere with the virus' ability to bind with a cell
•Some agents stimulate the body's immune system

Mechanism of Action (in combination or single action)

•Inhibit viral attachment

•Prevent genetic copying of virus
•Prevent viral protein production, which is vital for the reproduction of
the virus.[1]
Diagram on R: Schematic description of the mechanism of the four classes

of currently available antiviral drugs: fusion inhibitors (interfere with the

binding, fusion or entry of a virion), reverse-transcriptase inhibitors (interfere

with the translation of viral RNA into DNA), integrase inhibitors (block the

viral enzyme integrase, that inserts the viral genome into the DNA of the

host cell), protease inhibitors (block proteolytic cleavage of protein

precursors that are necessary for the production of infectious viral particles)
Virus Description

Viruses are obligate (i.e. by necessity) intracellular parasites.

•They lack both a cell wall and a cell membrane.

•They do not carry out metabolic processes.
•It must attach to and enter a host.
•It then uses the host cell's energy to synthesise protein, DNA and RNA
•A virus is difficult to kill as it lives inside the host's cell, and a drug that
kills the virus may also kill the cell[1].
Retroviruses are a type of virus in the viral family called Retroviridae.

Antiviral drugs target a diverse group of viruses, such as herpes, hepatitis,

and influenza viruses. On the other hand, antiretrovirals are drugs used to

treat retrovirus infections, the most common of which is HIV. Different classes

of antiretroviral drugs act on different stages of the HIV life cycle.[2].

There are many technical differences between viruses and retroviruses.

•Generally, the main difference between the two is how they replicate
within a host cell.
•Retroviruses use RNA as their genetic material and are named for a
special enzyme that’s a vital part of their life cycle — reverse
transcriptase (Transcription is the process in cells by which an enzyme
makes a copy of DNA from RNA. The enzyme that makes the DNA copy
is called reverse transcriptase and is found in retroviruses).
•The key steps that differentiate retroviruses from viruses are reverse
transcription and genome integration[2].