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Pharm > Antimalarial Drugs > Flashcards

Antimalarial Drugs Flashcards

1
Q

PLASMODIUM SPECIES

A
  • Plasmodium falciparum (majority of serious complications & deaths)
  • Plasmodium vivax
  • Plasmodium malariae
  • Plasmodium ovale
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2
Q

Symptoms and treatment of uncomplicated infection

A

Usual symptoms like fever, chills, diaphoresis, headaches, nausea and vomiting, body aches and general malaise

Treat with oral antimalarials

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3
Q

Symptoms and treatment of complicated infection

A

Symptoms: impaired consciousness /coma, severe normocytic anemia, renal failure, pulmonary edema, acute respiratory distress syndrome, circulatory shock, disseminated intravascular coagulation, spontaneous bleeding, acidosis, hemoglobinuria, repeated generalized convulsions, and/or parasitemia of >5%

Treat with parenteral (IV) antimalarials

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4
Q

BLOOD SCHIZONTICIDES

A 
CHLOROQUINE/ HYDROXYCHLOROQUINE QUININE/QUINIDINE
MEFLOQUINE
ARTEMISININ
LUMEFANTRINE 
ATOVAQUONE-PROGUANIL 
SULFADOXINE-PYRIMETHAMINE 
DOXYCYCLINE
CLINDAMYCIN
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5
Q

Which drug is the DOC for non-falciparum and sensitive uncomplicated falciparum malaria
• Preferred chemoprophylactic agent in areas without resistant falciparum malaria

A

CHLOROQUINE

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6
Q

Chloroquine is Highly effective against blood parasites but NOT active against _______

A

Highly effective against blood parasites But NOT active against liver stage parasites

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7
Q

Which drug

Prevents biocrystallization of hemoglobin breakdown product heme to non- toxic hemozoin, and thus causing parasite toxicity due to buildup of free heme

A

CHLOROQUINE

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8
Q

Pharmacokinetics and resistance of chloroquine

A

Pharmacokinetics
• Oral
• t1/2 = 3-5 days (only need to take once weekly)

Resistance
• P. falciparum: mutations in putative transporter, PfCRT* (P. falciparum Chloroquine Resistance Transporter)

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9
Q

This drug causes hemolysis in g6pd deficient patients and pruritus in Africans

A

Chloroquine

It is also contraindicated in people with :
• Psoriasis or porphyria (may precipitate attacks)
• Retinal or visual field abnormalities
SAFE IN PREGNANCY & YOUNG CHILDREN

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10
Q

Which drug is

Used as an alternative to chloroquine in chloroquine sensitive areas . Chemoprophylaxis and treatment of uncomplicated malaria

A

HYDROXYCHLOROQUINE

MOA: precise mechanism is unknown
• weak base and may exert its effect by concentrating in the acid
vesicles of the parasite inhibiting polymerization of heme
• can also inhibit certain enzymes by its interaction with DNA.

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11
Q

HYDROXYCHLOROQUINE

Adverse Effects

A
  • GI upset, nausea, vomiting, headache (MOST COMMON)
  • Itching
  • hemolysis (in G6PD deficient patients)
  • retinopathy , visual disturbances
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12
Q

HYDROXYCHLOROQUINE

Contraindications

A

• Psoriasis and known hypersensitivity to chloroquine

SAFE IN PREGNANCY & CHILDREN

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13
Q

Parenteral treatment of severe/complicated falciparum malaria

A

Quinidine

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14
Q

Oral treatment of falciparum malaria or uncomplicated malaria (alternative in chloroquine resistant areas)

A

Quinine

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15
Q

MOA OF QUININE & QUINIDINE

A

Intercalates into DNA, disrupting parasite’s replication and transcription

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16
Q

Quinine and quinidine adverse effects

A

CCHHHUB

  • Cinchonism: tinnitus, headache, nausea, dizziness, flushing & visual disturbances
  • Cardiotoxicity: QT prolongation Torsades de pointes
  • Hypersensitivity: skin rashes, urticaria, angioedema, bronchospasm
  • Hematologic abnormalities: hemolysis (G6PD deficiency), leukopenia, agranulocytosis, thrombocytopenia
  • Hypoglycemia: due to stimulation of insulin release
  • Uterine contractions: still used in treatment of severe falciparum malaria in pregnancy
  • Blackwater fever: hemolysis & hemoglobinuria (likely hypersensitivity reaction)
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17
Q

WHEN TO DISCONTINUE QUININE & QUINIDINE?

A
  • severe cinchonism
  • hemolysis
  • hypersensitivity
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18
Q

QUININE & QUINIDINE contraindications

A

AVOID IN PATIENTS WITH
• visual or auditory problems
USE WITH CAUTION IN PATIENTS WITH
• underlying cardiac abnormalities

19
Q 
QUININE & QUINIDINE
Should not be used concurrently with ?
• Can raise plasma levels of ? 
• Reduce dose in renal insufficiency
FDA Category C- however, benefits do often outweigh risks in complicated malaria
A

QUININE & QUINIDINE
Should not be used concurrently with mefloquine
• Can raise plasma levels of warfarin & digoxin
• Reduce dose in renal insufficiency
FDA Category C- however, benefits do often outweigh risks in complicated malaria

20
Q

This drug destroys asexual blood forms of malarial pathogens. It is effective against most strains of P. falciparum and P.vivax and the only medication recommended for chemoprophylaxis in pregnant women in chloroquine resistant areas

A

MEFLOQUINE

  • Last resort drug
  • Treatment of uncomplicated falciparum malaria (given with Artesunate)
21
Q

Pharmacokinetics of mefloquine

A
  • Oral only

* Elimination t1/2 = 20 days (weekly prophylactic dosing)

22
Q

Adverse effects and contraindications of mefloquine

A
  • Neuropsychiatric: Dizziness, loss of balance, ringing in the ears, anxiety, depression, hallucinations- MOST SERIOUS
  • GI upset, rash- seen in LOW doses (weekly dosing)
  • Leukocytosis, thrombocytopenia, elevated liver enzymes, arrhythmias- HIGH doses

Contraindications
• Patients with history of:
Epilepsy, psychiatric disorders, arrhythmias, cardiac conduction defects,sensitivity to related drugs
DO NOT co-administer with quinine or quinidine
SAFE in young children & pregnancy

23
Q

Artemisinin subtypes

A
  • Artesunate : oral, IV, IM, rectal
  • Artemether: oral, IM, rectal
  • Dihydroartemisinin: oral

Coartem = artemether + lumefantrine

24
Q

ARTEMISININ: MOA and pharmacokinetics

A

Binds iron leading to generation of free radicals

NOT used alone for chemoprophylaxis. If used alone, artesunate must be administered 5-7 days (otherwise recurrent parasitemia results)

25
Q

Which drug

  • Treatment of uncomplicated falciparum malaria in nearly all endemic areas
  • Treatment of severe falciparum malaria (given IV)
  • NO effect on hepatic stages
A

Artemisinin

- combination therapy protects against resistance and recrudescence

26
Q

Adverse effects of artemisinin

A

Neurotoxicity, QT prolongation- VERY HIGH DOSES

*IV Artesunate is used to treat severe malaria during ALL trimesters of pregnancy

27
Q

This drug is only used in combination with artemether

A

LUMEFANTRINE

28
Q

Which drug

disrupts mitochondrial electron transport and is given orally

A

ATOVAQUONE

- A component of a fixed dose formulation (+ Proguanil) known as Malarone

29
Q

Clinical Applications and antimalarials action of atovaquone

A

Clinical Applications
• Treatment & prophylaxis of chloroquine/ multi-drug resistant P. falciparum
• Alternative treatment of mild to moderate Pneumocystis jirovecii pneumonia

Antimalarial Action
• Active against tissue & erythrocytic schizonts
• Chemoprophylaxis can be started 1-2 days before travel and discontinued 1 week after exposure

Not advised in pregnant women

30
Q

Blood schizonticides that are folate synthesis inhibitors

A
  • Pyrimethamine
  • Proguanil
  • Sulfadoxine

Usually in combination

  • Pyrimethamine + Sulfadoxine
  • Proguanil + Atovaquone (Malarone)
  • Sulfadoxine + Pyrimethamine
31
Q

Clinical applications of folate synthesis

A

• Chemoprophylaxis
• Intermittent Preventive Therapy
• Treatment of chloroquine-resistant non-severe falciparum malaria
-Sulfadoxine + Pyrimethamine* can be used
* NO longer part of the CDC recommendation because of high-level of resistance
Other uses:
• Toxoplasmosis & Pneumocystis jirovecii (PCP) infection treatment

32
Q

FOLATE SYNTHESIS INHIBITORS MOA

A
33
Q

FOLATE SYNTHESIS INHIBITORS

Adverse Effects

A
  • Generally well tolerated
  • GI upset, rashes, itching, mouth ulcers, alopecia = RARE
  • Dermatologic reactions like erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis- SERIOUS but UNCOMMON
  • For sulfonamides, hematologic toxicity is RARE
34
Q

This drug is A tetracycline antibiotic: protein synthesis inhibitor by binding to 30s ribosome in susceptible microorganism

A

Doxycycline

35
Q

Clinical applications of doxycycline

A
  • Given with quinine in the treatment of uncomplicated falciparum malaria
  • Used to complete treatment for severe falciparum malaria after initial treatment with quinine, quinidine or artesunate
  • One of the recommended chemoprophylaxis for use in most malaria-endemic regions with chloroquine-resistant strains
36
Q

Adverse effects of doxycycline

A
  • GI upset, photosensitivity, candidal vaginitis
  • Discoloration & hypoplasia of teeth, stunting of growth
  • Fatal hepatotoxicity (in pregnancy)
  • DO NOT use in pregnancy or children < 8y/o (FDA Category D)
37
Q

This drug is

• used as an alternative to doxycycline
• Protein synthesis inhibitor, binds to the 50S ribosome subunit in susceptible microorganisms and blocks translocation
SAFE IN PREGNANCY & CHILDREN

A

Clindamycin

38
Q

Adverse effect of CLINDAMYCIN

A

pseudomembranous colitis (superinfection of C. dificile)

39
Q

Who are the TISSUE SCHIZONTICIDES

A

PRIMAQUINE

ATOVAQUONE-PROGUANIL

40
Q

DOC for eradication of dormant liver forms of P. vivax and P. ovale

A

Primaquine

41
Q

Clinical applications of primaquine

A
  • Radical cure of acute P. vivax and P. ovale malaria
  • Terminal prophylaxis of P. vivax and P. ovale malaria
  • Chemoprophylaxis of all species (good protection against P. falciparum & P.vivax (toxicities are a concern – reserved for when other drugs cannot be used)
  • Gametocidal against P. falciparum
  • Pneumocystis jirovecii pneumonia (PCP) alternative treatment
42
Q

Primaquine MOA and adverse effects

A

Acts as a cellular oxidant that disrupts metabolic processes of plasmodia mitochondria

Causes: Hemolysis or methemoglobinemia (especially in G6PD deficient patients)

AVOIDED IN PREGNANCY!
*Fetus is relatively G6PD deficient

43
Q

Primaquine oxidizes ____to _____

A

Primaquine oxidizes GSH to GSSG.

Therefore, less GSH is available to neutralize toxic compounds.

44
Q

Who are the gametocides

A

Primaquine

Pharm (8 decks)

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