Protozoal infections are caused by eukaryotic, unicellular protozoa and include diseases like malaria, amoebiasis, and giardiasis. They are often caused by unhygienic conditions and can be difficult to treat as anti-protozoal drugs are more toxic than antibiotics for bacterial infections. Malaria is caused by Plasmodium parasites and transmitted between humans and mosquitos. It has an asexual replication phase in humans and a sexual phase in mosquitos. Common antimalarial drugs include chloroquine, primaquine, mefloquine, atovaquone-proguanil, and artemisinin compounds.
Pharmacology of antimalarial drugs with treatment of malaria. mechanism of action, uses, adverse effects of antimalarial drugs like chloroquine, quinine, artemisinin compounds.
Pharmacology of antimalarial drugs with treatment of malaria. mechanism of action, uses, adverse effects of antimalarial drugs like chloroquine, quinine, artemisinin compounds.
Proton pump inhibitors (PPIs) block the gastric H,K-ATPase, inhibiting gastric acid secretion. This effect enables healing of peptic ulcers, gastroesophageal reflux disease (GERD), Barrett's esophagus, and Zollinger-Ellison syndrome, as well as the eradication of Helicobacter pylori as part of combination regimens.Proton-pump inhibitors (PPIs) are a class of medications that cause a profound and prolonged reduction of stomach acid production. They do so by irreversibly inhibiting the stomach's H+/K+ ATPase proton pump.[1]
They are the most potent inhibitors of acid secretion available.[2] Proton-pump inhibitors have largely superseded the H2-receptor antagonists, a group of medications with similar effects but a different mode of action, and antacids.[3]
PPIs are among the most widely sold medications in the world. The class of proton-pump inhibitor medications is on the World Health Organization's List of Essential Medicines.[4][5] Omeprazole is the specific listed example.[4][5]
Mechanism of action
The activation of PPIs
Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ATPase, or, more commonly, the gastric proton pump) of the gastric parietal cells.[71] The proton pump is the terminal stage in gastric acid secretion, being directly responsible for secreting H+ ions into the gastric lumen, making it an ideal target for inhibiting acid secretion.[citation needed]Because the H,K-ATPase is the final step of acid secretion, an inhibitor of this enzyme is more effective than receptor antagonists in suppressing gastric acid secretion.[72] All of these drugs inhibit the gastric H,K-ATPase by covalent binding, so the duration of their effect is longer than expected from their levels in the blood.[73]
Targeting the terminal step in acid production, as well as the irreversible nature of the inhibition, results in a class of medications that are significantly more effective than H2 antagonists and reduce gastric acid secretion by up to 99%.[2
The current slide include the pharmacology og cephalosporins.
Contents
Introduction to Cephalosporins
Classification of Cephalosporins
Cefazolin
Cephalexin
Cefuroxime
Cefuroxime axetil
Cefotaxime
Cefixime
Cefpodoxime proxetil
Cefepime
Adverse effects of Cephalosporins
Uses of Cephalosporins
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
Proton pump inhibitors (PPIs) block the gastric H,K-ATPase, inhibiting gastric acid secretion. This effect enables healing of peptic ulcers, gastroesophageal reflux disease (GERD), Barrett's esophagus, and Zollinger-Ellison syndrome, as well as the eradication of Helicobacter pylori as part of combination regimens.Proton-pump inhibitors (PPIs) are a class of medications that cause a profound and prolonged reduction of stomach acid production. They do so by irreversibly inhibiting the stomach's H+/K+ ATPase proton pump.[1]
They are the most potent inhibitors of acid secretion available.[2] Proton-pump inhibitors have largely superseded the H2-receptor antagonists, a group of medications with similar effects but a different mode of action, and antacids.[3]
PPIs are among the most widely sold medications in the world. The class of proton-pump inhibitor medications is on the World Health Organization's List of Essential Medicines.[4][5] Omeprazole is the specific listed example.[4][5]
Mechanism of action
The activation of PPIs
Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ATPase, or, more commonly, the gastric proton pump) of the gastric parietal cells.[71] The proton pump is the terminal stage in gastric acid secretion, being directly responsible for secreting H+ ions into the gastric lumen, making it an ideal target for inhibiting acid secretion.[citation needed]Because the H,K-ATPase is the final step of acid secretion, an inhibitor of this enzyme is more effective than receptor antagonists in suppressing gastric acid secretion.[72] All of these drugs inhibit the gastric H,K-ATPase by covalent binding, so the duration of their effect is longer than expected from their levels in the blood.[73]
Targeting the terminal step in acid production, as well as the irreversible nature of the inhibition, results in a class of medications that are significantly more effective than H2 antagonists and reduce gastric acid secretion by up to 99%.[2
The current slide include the pharmacology og cephalosporins.
Contents
Introduction to Cephalosporins
Classification of Cephalosporins
Cefazolin
Cephalexin
Cefuroxime
Cefuroxime axetil
Cefotaxime
Cefixime
Cefpodoxime proxetil
Cefepime
Adverse effects of Cephalosporins
Uses of Cephalosporins
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
an interesting and exhaustive presentation for medical undergraduates and postgraduates on antimalarial drugs... and also helpful to physicians for learning new concepts like ACT, for treating resistant malaria and knowing important ADR of antimalarial drugs..
Entropy in physics, biology and in thermodynamicsjoshiblog
Entropy is a measure of probability and the "disorder" of a system.
Disorder refers to is really the number of different microscopic states a system can be in, given that the system has a particular fixed composition, volume, energy, pressure, and temperature.
the exact definition is
Entropy = (Boltzmann's constant k) x logarithm of number of possible states
= k log(N).
The first law of thermodynamics defines the relationship between the various forms of energy present in a system (kinetic and potential), the work which the system performs and the transfer of heat.
We can imagine thermodynamic processes which conserve energy but which never occur in nature.
For example, if we bring a hot object into contact with a cold object, we observe that the hot object cools down and the cold object heats up until an equilibrium is reached. The transfer of heat goes from the hot object to the cold object.
According to the second law of thermodynamics, in any process that involves a cycle, the entropy of the system will either stay the same or increase. When the cyclic process is reversible then the entropy will not change. When the process is irreversible, then entropy will increases.
The second law states that there exists a useful state variable called entropy S. The change in entropy delta S is equal to the heat transfer delta Q divided by the temperature T.
delta S = delta Q / T
Order can be produced with an expenditure of energy, and the order associated with life on the earth is produced with the aid of energy from the sun.
For example, plants use energy from the sun in tiny energy factories called chloroplasts Using chlorophyll in the process called photosynthesis, they convert the sun's energy into storable form in ordered sugar molecules. In this way, carbon and water in a more disordered state are combined to form the more ordered sugar molecules.
In animal systems there are also small structures within the cells called mitochondria which use the energy stored in sugar molecules from food to form more highly ordered structures.
The long and winding road to chemical informationEngelbert Zass
8th German Conference on Chemoinformatics, Goslar, 12.11.2012 (Award address for the Gmelin-Beilstein-Denkmünze of the Gesellschaft Deutscher Chemiker)
Anti-malarial drugs [Drugs used for Malaria].pptx slide share Imad Agarwal
Malaria is major health problem in Pakistan and tropics. Malaria is caused by 4 species of plasmodium parasite.
☆ Plasmodium Vivax
☆ Plasmodium Ovale
☆ Plasmodium Falciparum
☆ Plasmodium Malaria
Chemically Anti-malarial drugs are classified to two categories. 4 aminoquinolines and 8 aminoquinolines.
1• 4 Aminoquinolines
Chloroquine, Amodiaquine, Piperaquine, Mefloquine, Quinine, Proguanil, pyrimathamine, and Sulfadoxine .
3•8 Aminoquinolines
Primaquine, Tafenoquine, Atovaquone, pyronarodin, Halofantrene, Lumefantrene, Artesunate, Artemether, Arteether and Arterolane.
#pharmacology #Nursing #Nursingnotes #antimalarial
Hello friends. In this PPT I am talking about antiprotozoal drugs. If you like it, please do let me know in the comments section. A single word of appreciation from you will encourage me to make more of such videos. Thanks. Enjoy and welcome to the beautiful world of pharmacology where pharmacology comes to life. This video is intended for MBBS, BDS, paramedical and any person who wishes to have a basic understanding of the subject in the simplest way.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
263778731218 Abortion Clinic /Pills In Harare ,sisternakatoto
263778731218 Abortion Clinic /Pills In Harare ,ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group of receptionists, nurses, and physicians have worked together as a teamof receptionists, nurses, and physicians have worked together as a team wwww.lisywomensclinic.co.za/
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
1. Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
2. Protozoa are eukaryotes and unicellular organisms.
Most of the protozoal infections are due to unhygienic
conditions.
Less easily treated than bacterial infections and
antiprotozoal drugs are more toxic.
Protozoal infections may be one or more infection
results from the following:
Amoebiasis, trypanosomiasis, giardiasis, leishmaniasis,
trichomoniasis, Malaria, toxoplasmosis.
PROTOZOAL INFECTIONS
3. Plasmodium species which infect
humans
Plasmodium vivax (tertian):
Plasmodium ovale (tertian)
Plasmodium falciparum (M.tertian)
Plasmodium malariae (quartan)
9. Synthesized by Germans in 1934 ( resochin)
d & l isomers, d isomer is less toxic
Cl at position 7 confers maximal antimalarial efficacy
Antimalarial activity:
High against erythrocytic forms of vivax, ovale,
malariae & sensitive strains of falciparum
Gametocytes of vivax
10. Hemoglobin Globin utilized by
malarial parasite
Heme (highly toxic for malaria parasite)
Chloroquine
Quinine, (+) Heme Polymerase
mefloquine
Lumifantrine
pyronaridine (-)
Hemozoin (Not toxic to plasmodium)
11. Other parasitic infections:
Giardiasis, taeniasis, extrainstestinal amoebiasis
Other actions:
Depressant action on myocardium, direct relaxant effect
on vascular smooth muscles, anti-inflammatory,
antihistaminic , local anaesthetic
Resistance develops due to efflux mechanism
Well absorbed, tmax 2-3 hrs , 60 % protein bound
Concentrated in liver , spleen, kidney, lungs , leucocytes
Selective accumulation in retina: ocular toxicity
T1/2 = 3-10 days increases from few days to weeks
12. Chloroquine is administered in loading
dose in malaria
Chloroquine is well absorbed after oral administration.
It is extensively tissue bound and sequestrated by
tissues particularly liver, spleen, kidney it has got large
apparent volume of distribution
So it is given in loading dose to rapidly achieve the
effective plasma conc.
600 mg of base stat
300 mg base after 8 hours
150 mg of base BD for 2 days
200 mg oral tablet of chloroquine phosphate consists
of 150 mg base
13. Intolerance:
Nausea, vomiting, anorexia
skin rashes, angioneurotic edema, photosensitivity,
pigmentation, exfoliative dermatitis's
Long term therapy may cause bleaching of hair
Rarely thrombocytopenia, agranulocytosis,
pancytopenia
14. Ocular toxicity: High dose prolonged therapy
Temporary loss of accommodation
Lenticular opacities, sub capsular cataract
Retinopathy: constriction of arteries, edema, blue
black pigmentation , constricted field of vision.
CNS: Insomnia, transient depression seizures,
rarely neuromyopathy & ototoxicity
CVS: ST & T wave abnormalities, abrupt fall in BP &
cardiac arrest in children reported
16. HYDROXY CHLOROQUINE:
Less toxic, properties &uses similar
AMODIAQUINE:
As effective as chloroquine
Pharmacological actions similar
May be effective in Chloroquine resistant strains
Adverse events: GIT, headache , photosensitivity,
rarely agranulocytosis
Not recommended for prophylaxis
Pyronaridine: effective in resistant cases
4 AMINOQUINOLINES:
17. 1820 Pelletier & caventou isolated quinine from
cinchona bark.
Mechanism of action:
Similar to chloroquine
‘General protoplasmic poison’
Pharmacokinetics-Administered orally is completely
absorbed
Tmax = 1-3 hrs , crosses placental barrier
Metabolized in liver degradation products excreted in
urine t ½ = 10 hrs
18. Antimalarial action:
Erythrocytic forms of all malarial parasites including
resistant falciparum strains .
Gametocidal for vivax & malariae
Local irritant effect: Local pain sterile abscess.
3. Cardiovascular: depresses myocardium, ↓ excitability,
↓ conduc vity, ↑ refractory period, profound
hypotension IV.
4. Miscellaneous actions: Mild analgesic, antipyretic
activity , stimulation of uterine smooth muscle, curare
mimetic effect
19. Malaria:
uncomplicated resistant falciparum malaria
Cerebral malarial
Myotonia congenita: 300 to 600 mg BD/ TDS
Nocturnal muscle cramps: 200 – 300 mg before
sleeping
Spermicidal in vaginal creams
Varicose veins: along with urethane causes thrombosis
& fibrosis of varicose vein mass
21. Idiosyncrasy : similar to Cinchonism but occurs in
therapeutic doses-pruritis, urticaria, hemolytic anemia
and agranulocytosis
Cardiovascular toxicity: cardiac arrest, hypotension
fatal arrhythmias
Hypoglycemia
Black water fever-intravascular hemolysis,
hemoglobinuria, fever and acute renal failure
22. Primaquine-Converted to electrophiles Generates
reactive oxygen species
Liver Hypnozoites
Weak action against erythrocytic stage of vivax, so
used with suppressive in radical cure
No action against erythrocytic stage of falciparum
Has gametocidal action and is most effective
antimalarial to prevent transmission disease against all
4 species
23. Readily absorbed,
t1/2 = 3-6 hrs
Oxidized in liver
excreted in urine
Uses-Primary use is radical cure of relapsing malaria 15
mg daily for 14 days with dose of chloroquine
Falciparum malaria 45 mg of single dose with
chloroquine curative dose to kill gametes & cut down
transmission of malaria.
25. Tafenoquine:
More active slowly metabolized analog of
primaquine, has advantage that it can be given on
weekly basis.
Tried for radical cure in 3 days
Bulaquine:
Congener of primaquine developed in India
Comparable antirelapse activity when used for 5
days
Partly metabolized to primaquine
Better tolerated in G6PD deficiency
Tafenoquine and Bulaquine
26. Quinoline methanol derivative developed to deal with
chloroquine resistant malaria and MDR-Muti Drug
resistant species
Rapidly acting erythrocytic schizonticide, slower than
chloroquine & quinine
Mechanism of action similar to chloroquine
Neither gametocidal, nor kills Hypnozoites
27. Good but slow oral absorption
High protein binding
Concentrated in liver, lung, intestine
Extensive metabolism in liver, primarily secreted in
bile , under goes enterohepatic circulation
Long t1/2 = 2 – 3 weeks
Caution- minimum of 12hr interval after quinine
administration as both are cardiotoxic
28. Effective drug for MDR falciparum
T/t of uncomplicated falciparum in MDR malaria
should be used along with Artesunate (ACT)
Prophylaxis in MDR areas 250 mg per week started 2-
3 weeks before to assess side effects
Due to fear of drug resistance mefloquine should not
be used as drug for prophylaxis in residents of endemic
area
30. Quinoline methanol
Used in chloroquine resistant malaria since 1980
Erratic bioavailabilty, lethal cardiotoxicity & cross
resistance to mefloquine limited its use
Now a days used only when no other alternative
available can act against chloroquine, quinine and
pyrimethamine resistant strains
Adverse events; Nausea, vomiting, QT prolongation ,
diarrhoea, itching , rashes
C/I: along with quinine, chloroquine, antidepressants,
antipsychotics.
31. Synthetic naphthoquinone
Rapidly acting erythrocytic schizonticide for
plasmodium falciparum & other plasmodia
MOA: Collapses mitochondrial membrane & interferes
ATP production
Proguanil potentiates action of atovaquone and
prevents development of resistance
Also used in P. Jiroveci & Toxoplasma gondi infections
32. Proguanil :
Biguanide converted to cycloguanil active compound
Act slowly on erythrocytic stage of vivax &
falciparum
Prevents development of gametes
Adverse effects:
Stomatitis, mouth ulcers, larger doses cause
depression of myocardium, megaloblastic anemia
Not a drug for acute attack
Causal prophylaxis: 100 – 200 mg daily
33. Pyrimethamine is diaminopyrimidine more potent than
proguanil & effective against erythrocytic forms of all
species, toxoplasmosis, polycythemia vera
Inhibits dihydrofolate reductase enzyme
Tasteless so suitable for children
Used in uncomplicated chloroquine resistant malaria
Sulfadoxine(1500mg)+ Pyrimethamine(75mg)-single dose
Adverse events: sulfa related
megaloblastic anemia, thrombocytopenia,
agranulocytosis.
34. Artemisinin is the active principle of the plant
Artemisia annua
Sesquiterpene lactone derivative
Most potent and rapid acting blood schizonticides
Short duration of action
Poorly soluble in water & oil
Artesunate
Artemether
Arteether
Arterolane
35. These compounds have presence of endoperoxide
bridge
Endoperoxide bridge interacts with heme in parasite
Heme iron cleaves this endoperoxide bridge
There is generation of highly reactive free radicals
which damage parasite membrane by covalently
binding to membrane proteins
36. MOA-
2) Artemisinin free radicals specifically inhibit a plasmodial
sarcoplasmic-endoplasmic calcium ATPase
Water soluble ester of dihydroartemisinin
Dose: can be given oral, IM,IV, rectal t1/2- 1-2hrs
Oral -100 mg BD on day 1, 50 mg BD day 2 to day 5
Parenteral-120 mg on day 1 (2.4 mg/kg BD )
60 mg OD ( 2.4 mg/kg) for 7 days
Artemisinin
Artemisinin
Conventional
Treatment
37. Methyl ether of dihydroartemisinin
Converted to DHA-dihydroartemisinin, not given IV, t1/2-3-10hrs
Dose: Oral & IM-80 mg BD on day 1 (3.2 mg/kg)
80 mg OD (1.6 mg/kg) for 7 days
ARTEETHER –
Ethyl ether of dihydroartemisinin
Therapeutically equivalent to quinine in cerebral malaria
A longer t1/2 & more lipophilic than artemether favoring
accumulation in brain
Given IM only T1/2-23hrs
Dose:3.2 mg/kg on day1 followed by 1.6 mg/kg daily for next 4
days
ARTEROLANE-available for oral use only in combination
38. Leucopenia
Hypersensitivity: Drug fever, itching
GIT: nausea, vomiting, abdominal pain (common)
ECG changes: ST-T changes, QT prolongation
Abnormal bleeding, dark urine
Reticulocytopenia
D/I-concurrent administration with astemizole,
antiarrhythmics, tricyclic antidepressants and
phenothiazines increase the risk of cardiac conduction
defects
39. Artemisinin compounds are shorter acting drugs
Monotherapy needs to be extended beyond
disappearance of parasite to prevent recrudescence
This can be prevented by combining 3-5 day regimen of
Artemisinin compounds with one long acting drug like
mefloquine 15 mg/kg single dose
Indicated by WHO in acute uncomplicated resistant
falciparum malaria
Rapid clinical & parasitological cure
High cure rates and low relapse rates
40. There are now more trials involving Artemisinin and its derivatives than
other antimalarial drugs, so although there are still gaps in our
knowledge, there is a reasonable evidence base on safety and efficacy
from which to base recommendations.
Combinations which have been evaluated:
piperaquineArtemisinin +
mefloquine
Artesunate +
piperaquinedihydroartemisinin +
mefloquine
lumefantrineartemether +
mefloquine
naphthoquine
chloroquine
amodiaquine
sulfadoxine-
pyrimaethaminine
mefloquine
proguanil-dapsone
chlorproguanil-dapsone
atovaquone-proguanil
clindamycin
tetracycline
doxycycline
41. Indication:
Duration :1-2 weeks before to 4 weeks after
returning from endemic area
Drug regimens:
Chloroquine sensitive malaria: 300 mg / week
Chloroquine resistant malaria:
Mefloquine 250 mg once a week ,
Doxycycline 100 mg daily ,
Atovaquone + Proguanil daily
42. Quinine ,
Artemisinin compounds
Pyrimethamine sulfadoxine
Amodiaquine
Drugs used in chloroquine resistant malaria
Mefloquine
Quinine
Sulfadoxine pyrimethamine
Artemisinin compounds
43. Lumefantrine is highly effective, long acting oral
erythrocytic schizonticide related to mefloquine
MOA- similar to chloroquine
-also affects nucleic acid and protein synthesis of parasite
Fatty food increases absorption
Highly lipophilic onset delayed ,
peak 6 hrs
Available as fixed dose combination
80 mg artemether bd with 480 mg lumefantrine bd for 3
days
44. Tetracyclines and doxycycline
Slow but potent action on erythrocytic stage of all MP
& Pre-erythrocytic stage of falciparum
Always used in combination with quinine or S-P for
treatment of chloroquine resistant malaria
CLINDAMYCIN
Bacteriostatic antibiotic, erythrocytic schizontocide
Potentiates the action of quinine and artemisinin
45. Tab. Chloroquine phosphate 250 mg
Contains 150 mg of base
Give 4 tablets stat , 2 tablets after 8 hours and , 1
tablet BD for 2 days
Patients who cannot take orally
3.5 mg/kg IM every 6 hrs for 3 days
Tab primaquine 15 mg OD for 14 days in Plasmodium
vivax, ovale
Primaquine 45 mg single dose for falciparum after
chloroquine (gametocidal)
46. Pts who can take orally:
3 tablets of (Pyrimethamine + sulfadoxine) single dose
followed by quinine 600 mg TDS for 2 days or
Tab Quinine 600 mg TDS X 3 days with Cap
doxycycline 100 mg BD for 7 days or
Quinine 3 days with mefloquine or
(Atovaquone 250 mg + Proguanil 100 mg) 4 tab(Single
dose ) for 3 days or
Artesunate 100 mg BD x 3 days with Sulfadoxine-
Pyrimethamine or mefloquine
47. Pts who cannot take orally
Inj Quinine Hcl 20 mg/kg in 500 ml dextrose saline
over 4 hrs then
10 mg/kg in dextrose saline over 2 hrs every 8 hrly
till patient is able to swallow
Then quinine 600 mg TDS for 7 days & tetracycline/
doxycycline
Or
Artemether / Arteether injection
Chloroquine resistant malaria
48. Artesunate 2.4 mg/kg IV/IM, BD on day1 then 2.4
mg/kg daily for 7 days OR
Artemether 3.2 mg/kg IM on day 1 then 1.6 mg/kg
daily for 7 days OR
Arteether 3.2 mg/kg IM on day1, followed by 1.6
mg/kg daily for next 4 days
Switchover to 3 Day oral ACT in between whenever
patient can take oral medication
49. Quinine: 20 mg quinine salt/kg on admission
(i.v. infusion in 5% dextrose/dextrose saline over a
period of 4 hours) followed by maintenance dose of 10
mg/kg body weight 8 hourly.
When ever patient can swallow orally switch over to
oral quinine 10 mg/kg 8 hrly and complete 7 days
course
50. Quinine parenteral high toxicity / oral well tolerated
Primaquine avoided in neonates
Mefloquine not used in children below 15 kg weight
Acute malaria in pregnant women
Chloroquine in usual doses
Mefloquine C/I in first trimester
Primaquine/ tetracycline avoided
Anemia: folic acid & iron
Malaria in children