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Pharmacology -- Test #2 > Antiparasitics #1 -- Malaria > Flashcards

Antiparasitics #1 -- Malaria Flashcards

1
Q

Name the five human malaria parasites

A 
Plasmodium falciparum
Plasmodium vivax
Plasmodium ovale
Plasmodium malariae
Plasmodium knowlesi
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2
Q

Which malaria parasite is responsible for the most deaths?

A

Plasmodium falciparum

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3
Q

Which malarias are known to be relapsing?

A

Vivax and Ovale

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4
Q

What causes malaria relapse?

A

Hypnozoites in the liver

In vivax can stay for weeks-months

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5
Q

Describe the life cycle of Plasmodium falciparum.

A
  1. Mosquito Bite
  2. Sporozites from bite form merozoites in liver
  3. These invade RBCs and mature to trophozoite
  4. Multiply, make mero., released with RBC rupture
  5. Some meros become gametocytes, taken up by mosquito.

Circle of life and shit.

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6
Q

How does cerebral malaria happen

A

Occlusions of vessels outside of capillary beds

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7
Q

What makes malaria especially dangerous in pregnant women

A

It binds chondroitin sulfate A allowing it to latch onto the placenta

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8
Q

Primoquine is an important malarial drug because it…

A

targets the liver stage

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9
Q

Classic symptoms of uncomplicated malaria?

A

Cold Stage
Hot Stage
Sweating Stage
48 hour periodicity for Falciparum + Vivax

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10
Q

Less Classic symptoms of malaria

A

Fever + Flu-like symptoms
Chills, Headache, Myalgias, and Malaise
Anemia and Jaundice

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11
Q

What do you see in severe malaria cases (5)…

A 
Organ failures (esp. kidney)
Cerebral Malaria
Severe Anemia and hemoglobinuria
Acute Respiratory Distress Syndrome
Placental Malaria
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12
Q

What is seen in a cerebral malaria patient?

A 
Abnormal behavior
Impairment of consciousness
Seizures
Coma
Other neurologic abnormalities
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13
Q

Cause of hemoglobinuria in malaria?

A

hemolysis

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14
Q

Placental malaria is especially common with….

A

first pregnancy

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15
Q

Three types of antimalarial drugs

A

Tissue schizonticides
Blood schizonticides
Gametocytocides

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16
Q

What is a Schizont

A

The malarial form between trophozoite and merozyte

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17
Q

What do tissue schizonticides do?

A

Kill liver stage parasites

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18
Q

What do blood schizonticides do?

A

Kill erythrocytic forms

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19
Q

What do gametocytes for malaria do

A

Kill sexual stages of the parasite to block transmission

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20
Q

How to not get malaria?

A

Insect repellants
Insecticides
Bed Nets
Chemoprophylaxis

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21
Q

Factors that may influence choice of chemoprophylactic?

A

Species present
Level and type of drug resistance
Lead time before travel

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22
Q

Malarone is made of…

A

Atovaquone + Proguanil

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23
Q

Where is Malaron effective?

A

All areas

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24
Q

Timeline for Malaron dosing

A

Start 1-2 days prior, continue 7 days after

Daily administration

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25
Q

Where is Doxycycline effective?

A

All areas

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26
Q

Timeline for doxycycline dosing

A

Start 1-2 days prior, continue for 4 weeks

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27
Q

What is Chloroquine comprised of?

A

Aralen and generic

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28
Q

Where is Chloroquine effective?

A

Chloroquine sensitive areas

Preferred in Central and South America

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29
Q

Chloroquin dosing timeline.

A

Start 1-2 weeks prior and continue 4 weeks after out of area

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30
Q

What is Mefloquine comprised of?

A

Lariam and generic

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31
Q

Where is Mefloquine effective?

A

Mefloquine sensitive areas

Whoops – Note taking fail – sorry gang

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32
Q

Timeline of mefloquine dosing.

A

Start more than 2 weeks early and continue for 4 weeks

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33
Q

Important reason to start doing with Mefloquine early

A

You want to take it long enough to establish a high enough concentration to reveal any toxicity symptoms before traveling abroad

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34
Q

Perks of Mefloquine

A

Taken once per week

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35
Q

When is Primaquine usually given?

A

Its given if an area is comprised to 90% Plasmodium vivax

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36
Q

Timeline for Primaquine dosing.

A

Start 1-2 days prior and continue for 7 days after

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37
Q

Important considerations when evaluating treatment options for malaria

A

Type of infecting parasite
Area where infection was acquired/drug resistant status
Clinical Status of Patient

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38
Q

What components of the clinical status of the patient are important guides in gauging clinical options

A

Accompanying illness/condition (G6PD deficient)
Pregnancy
Drug Allergies
Other Meds that may cross react

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39
Q

In a case of uncomplicated malaria/unidentified species contracted in a chloroquine sensitive area, how would you treat

A

Chloroquine (Aralen) and Hydroxychloraquine sulfate (Plaquenil)

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40
Q

In a case of uncomplicated malaria/unidentified species contracted in a chloroquine resistant area, how would you treat

A

Malarone (Atovaquone + Proguanil)
Coartem (Artemether + lumefantrine)
Quinine Sulfate + (Doxy, tetracycline, or clindamycin)
Mefloqine (Lariam)

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41
Q

What is Coartem?

A

Artemether + lumefantrine

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42
Q

Treatment of uncomplicated malaria with P. vivax or P. ovale infection (hypnozoites in liver) in a CQ sensitive area

A

Chloroquine OR

Hydroxychloroquine + Primaquine

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43
Q

Treatment of uncomplicated malaria with P. vivax or P. ovale infection (hypnozoites in liver) in a CQ resistant area

A

Quinine Sulfate + (Doxy or tetra) + Primaquine
Malarone + Primaquine
Mefloquine + Primaquine

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44
Q

Treatment of uncomplicated malaria with P. marariae or P. knowlesi

A

Chloroquine or Hydroxychloroquine sulfate (Plaquenil)

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45
Q

Symptoms of Severe Malaria

A

Impaired consciousness/coma, severe normocytic anemia, renal failure, pulmonary edema, etc.

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46
Q

Go To Treatment for complicated malaria

A

Quinidine gluconate (IV) + (Doxy/Tetra/Clinda)

47
Q

When giving quinidine gluconate, what do you need to be watching out for?

A

Blood pressure – hypotension
Cardiac function – Widening of the QRS complex or lengthening of the QT interval
Blood Glucose - hypoglycemia

48
Q

If you can’t get ahold of quinidine gluconate, what should you give a complicated malaria patient?

A

Artesunate (IV)

49
Q

Artesunate should be followed by…

A

Malarone
Doxy (Clinda for preggers)
Mefloquine

50
Q

So what is artemisinin anyway?

A

Sesquiterpene lactone endoperoxide

51
Q

T or F. Artemisinin is a potent and fast acting drug

A

T. 10,000 fold reduction in 48 hours

52
Q

Resistance to Artemisinin is observed where…

A

SE Asia

53
Q

How does Artemisinin work?

A

Rapidly activing schizonticide
Activated by heme iron
May form free radicals that target parasite proteins and lipids

54
Q

How have parasites adapted to resist Artemisinin?

A

Mutations in Kelch 13

Delays progress through the life cycle, may alter the stress response

55
Q

Effect of artemisinin on liver stages of malaria

A

None

56
Q

Why is Artemisinin inappropriate for chemoprophylaxis?

A

It has a short half life (1-2 hours) that would require constant dosing
Leaves high recrudescence rates if used alone

57
Q

How can Artemisinin be made prophylactically useful?

A

Pairing with other drugs like Mefloquine or lumefantrine

58
Q

Two effects of the insolubility of artemisinin

A

Only used orally

low bioavailability

59
Q

How can artemisinin be made to be dosed in other routes?

A

Semisynthetic artemisinins can be given orally, intramuscularly, IV, and rectally – which is very imortant in severe cases.
Ex. Artesunate

60
Q

Top Five Artemisinin derivatives

A 
Artemininin
Dihydroartemisinin
Artemether
Arteether
Artesunate
61
Q

Is Artemisinin more effective as a bolus or infusion

A

bolus

62
Q

Describe Artemisinin combination therapy

A

Artemisinin bolus provides rapid knockdown

Longer half-life drugs eliminate remaining parasites

63
Q

Longer halflife drugs commonly used in artemisinin combination therapyq

A

Lumefantrine (Coartem)
Amodiaquine
Mefloquine
Piperaquine

64
Q

Adverse effects of Artemisinin?

A

Nausea, Vomiting, Diarrhea, Dizziness

Embryotoxic in animal studies

65
Q

Who are the three 4-aminoquinolines?

A

Quinine
Chloroquine (Aralen)
Mefloquine (Lariam)

66
Q

How do malaria parasites eat normally?

A

They ingest hemoglobin from host and degrade it into amino acids and free heme. Then the parasite polymerizes the heme into hemozoin to prevent free heme toxicity.

67
Q

How does chloroquine work?

A

Accumulates in food vacuole, inhibits heme polymerization

68
Q

How is chloroquine resistance developed

A

Lack of accumulation of chloroquine in the vacuole

69
Q

PK details about Chloroquine?

A

Formulated for oral use
Well absorbed
Large Vd
Half-life of 3-5 days, terminally 1-2 months

70
Q

Chloroquine – more effective as bolus or infusion?

A

Infusion

Maintaining Concentration for the win.

71
Q

Adverse effects of chloroquine

A

IN HEALTHY FOLKS

usually nothing, sometimes Pruritis

72
Q

Chloroquine is contraindicated in which patients?

A

Psoriasis, Porphyria
Retina/Visual Field Abnormalities
Myopathy
Glucose 6PD

73
Q

______ and ______ interfere with chloroquine absorption

A

Kaolin (antidiarrheal agent) and antacids

74
Q

Two mutations associated with CQ resistance

A

PfCRT1

PfMDR1

75
Q

What does PfCRT1 mutation do?

A

Caused reduced accumulation of chloroquine in the food vacuole
No cross resistance with mefloquine or quinine

76
Q

What does overexpression of PfMDR1 do?

A

Over expression of drug transporter pumps out the anti-malarials

77
Q

Quinine acts as which kind of medication?

A

Blood schizonticide

78
Q

Quinine is the treatment of choice for…

A

CQ resistant F. malaria (use quinine sulfate orally)

Severe F. malaria (use quinidine gluconate by IV)

79
Q

Why is Quinine inappropriate for chemoprophylaxis?

A

Shorter half life and toxicity

80
Q

Adverse effects of quinine

A

Cinchonism
Can stimulate uterine contractions
Hemolysis
Severe hypotension if infused too quickly

81
Q

What is cinchonism?

A

Tinnitis, headache, dizziness, flushing, and visual disturbances

82
Q

Hemolysis following Quinine dose is associated with…

A

G6PD deficiency

Blackwater fever

83
Q

What is blackwater fever?

A

Rare, Severe, Marked by hemoglobinuria

84
Q

Quinine is metabolized by…

Who the fuck cares?

A

CYP3A4

People on Warfarin and Digoxin care

85
Q

Which drug gives Elliot hypersexual dreams?

A

Mefloquine

86
Q

Is mefloquine used for prophylaxis or treatment?

A

Both.

87
Q

Mefloquine is effective against which malarial strains

A

P. falciparum, and P. vivax

88
Q

Adverse effects of Mefloquine.

A

Neuropsychiatric toxicity (seizures, toxic psychosis, sleep disturbance)

89
Q

Other than the big three, who are some super lame less important chloroqine related compounds

A

Lumefantrine
Piperaquine
Amodiaquine
Halofantrine

90
Q

What is Primaquine’s chemical name?

What kind of drug is it.

A

8-aminoquinoline

Pro-drug

91
Q

Which CYP metabolizes Primaquine

A

CYP 2D6

92
Q

Primaquine is the drug of choice for..

A

Liver stages (actively growing and hypnozoites) of P. vivax and P. Ovale (Combine with CQ)

93
Q

How does Primaquine work?

A

Gametocidal against all four parasites

94
Q

Contraindications for Primaquine.

A 
G6PD deficiency
Pregnancy
Breast Feeding
Granulocytopenia
Taking hemolytic drugs
95
Q

Related compound to primaquine that was apparently important enough to bring up, but all of the details on it are essentially “ditto on primaquine”

A

Tafenoquine

96
Q

Malarone is made of _____ and _____ because

A

Proguanil and Atavaquone

Resistance to Atavaquone happens really quickly if used as monotherapy

97
Q

Malarone kills…

A

Liver + Blood Stages

Not Hypnozoites

98
Q

Malarone is effective for….

A

Uncomplicated malaria

Chemoprophylaxis

99
Q

Atavaquone is also used to treat….

A

Toxoplasma gondii

Pneumocystis jiroveci

100
Q

How does Atavaquone work?

A

It is a selective inhibitor of malaria mitochondrial cytochrome bc1 complex. It inhibits electron transport and causes the mitochondrial membrane potential to collapse.

101
Q

What’s the point of mitochondrial electron transport in P. falciparum anyway?

A

To regenerate ubiquinone – which acts as an electron acceptor for parasite dihydroorotate dehydrogenase – which is essential for pyrimidine synthesis in the parasite.

102
Q

How does Proguanil work?

A

In the body, it is converted to cycloguanil, a selective inhibitor of thymidylate synthetase. This enzyme is crucial for parasite purine and pyramidine synthesis.

It also enchances mito. toxicity of atavaquone

103
Q

What is Thimidylate Synthetase

A

a bifunctional plasmodial dihydrofolate reductase

104
Q

What is Pyrimethamine-Sulfadoxine (Fansidar)?

A

A folate synthesis inhibitor that acts as a slow acting erythrocytic schizonticide

105
Q

How does primathamine work?

A

It inhibits plasmodia DHF-reductase, preventing pruduction of purines, thymidine

106
Q

How does sulfadoxine work?

A

It inhibits the activity of dihydropteroate synthase, preventing production of purines and thymidines

107
Q

Why is it idiotic that we are taking the time to cover Fansidar?

A

Because resistance is so common that this drug basically isn’t used anymore.

108
Q

Other than malaria, what might you treat with antifolates?

A

Toxoplasmosis (pyrimethamine+sulfadizine)

Pneumocystis (Trimethoprim+sulfamethoxazole)

109
Q

Why shouldn’t you use single anti-folates?

A

Resistance develops easily

Pairing allows lots of synergistic effects that allow lower doses

110
Q

Antibiotics commonly used as anti-malarial drugs

A

Tetracycline, Doxycycline, and Clindamycin

111
Q

How do antibiotics work against malaria?

A

Target components of the apicoplast

112
Q

What the fuck is an apicoplast anyway?

A

Plant-like organelle that carries out many biochemical processes

113
Q

Doxy is commonly pairs with ____ or _____ for freatment of F malaria

A

Quinine or Quinidine

114
Q

Where might Doxy be used for prophylaxis

A

Areas with high resistance to mefloquine

Pharmacology -- Test #2 (13 decks)

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