Antivirals, Antimalarials, and Anthelmintics

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Pharmacology
Chapter 33
Unit X, Chapter 33
updated 9 years ago by jncanf
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1

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

vidarabine (Vira-A)

FIRST INTRODUCED AS AN ANTINEOPLASTIC DRUG FOR TREATMENT OF LEUKEMIA. IN 1964 IT WAS DISCOVERED THAT IT EXERTS AN ANTIVIRAL EFFECT AGAINST HSV-1, HERPES ZOSTER, VARICELLA ZOSTER, AND CMV. NOT EFFECTIVE AGAINST HSV-2, GENITAL HERPES, IT HAS BEEN USED EFFECTIVELY TO TREAT HERPES SIMPLEX VIRAL ENCEPHALITIS.

2

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

amantadine HCl (Symmetrel)

ORIGINALLY TREATED PARKINSONISM; DOES NOT TREAT INFLUENZA B.
ROUTE AND DOSAGE:
INFLUENZA A: A < 65Y/C >9: PO: 200 MG/D IN 1 TO 2 DIVIDED DOSES.
OLDER ADULTS: > 65 Y: 100 MG/D
C: 1 TO 8 Y: PO 5 MG/KG/D IN 2 DIVIDED DOSES.

USES AND CONSIDERATIONS:
PRIMARY USE IS PROPHYLAXIS AGAINST INFLUENZA A. WELL ABSORBED BY GI TRACT. PREGNANCY CATEGORY: C; PB: UK; t1/2 24H

3

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS)"

amantadine HCl (Symmetrel)

SIDE EFFECTS AND ADVERSE REACTIONS:

SIDE EFFECTS AND ADVERSE REACTIONS:
CNS EFFECTS SUCH AS INSOMNIA, DEPRESSION, ANXIETY, CONFUSION, AND ATAXIA. ORTHOSTATIC HYPOTENSION; NEUROLOGIC PROBLEMS, SUCH AS WEAKNESS, DIZZINESS, AND SLURRED SPEECH; AND GI DISTURBANCES. SUCH AS ANOREXIA, NAUSEA, VOMITTING AND DIARRHEA.

4

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

cidofovir (Vistide)

DOES NOT TREAT INFLUENZA B;
ROUTE AND DOSAGE:
A: IV- 5 MG/KG IN 100 mL NS OVER 60 MIN. ONCE/WEEK FOR 2 WK. THEN 3 TO 5 MG/KG EVER OTHER WEEK. TAKE PROBENECID 2 G, 3 H BEFORE INFUSION, AND TAKE 1 G, 8 H AFTER INFUSION.

USES AND CONSIDERATIONS:
FOR CMV RETINITIS, ESPECIALLY IN CLIENTS WITH AIDS, KIDNEY DAMAGE MAY OCCUR; MONITOR KIDNEY FUNCTION; PREGNANCY CATEGORY: C; PB: UK, t1/2 - 17 TO 65 H.

5

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

foscarnet (Foscavir)

TREAT HIV-RETINITIS AND HERPES SIMPLEX INFECTION IN PEOPLE WITH AIDS.
ROUTE AND DOSAGE:
CMV RETINITIS:
A: IV 60 MG/KG INFUSED OVER 1 HOUR, Q8H, FOR 2 TO 3 WEEKS, OR 90 MG/KG/D INFUSED OVER 2 H, Q12H

USES AND CONSIDERATIONS:
FOR HERPESVIRUSES (HSV-1 AND HSV-2) AND CMV RETINITIS. CAN CAUSE KIDNEY DAMAGE AND HYPERPHOSPHATEMIA. CLOSELY MONITOR KIDNEY FUNCTION. DOES NOT CAUSE GRANULOCYTOPENIA OR THROMBOCYTOPENIA. PREGNANCY CATEGORY: C; PB: UK; t1/2 3 TO 4 H.

6

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

rimantadine HCl (Flumadine)

ROUTE AND DOSAGE:
A/C > 10 Y; PO 100 MG b.i.d.
C: < 10 Y ; PO 5 MG/KG.D; MAX: 150 MG/D
OLDER ADULTS: PO 100 MG/D

USES AND CONSIDERATIONS:
FOR PROPHYLAXIS AND TREATMENT AGAINST INFLUENZA A VIRUS. DRUG DOSE IS USUALLY REDUCED FOR CLIENTS WITH SEVERE HEPATIC OR RENAL IMPAIRMENT. PREGNANCY CATEGORY: C; PB: 40%, t1/2 33 H
*CNS SIDE EFFECTS OF RIMANTADINE OCCUR LESS OFTEN THAN WITH AMANTADINE.

7

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

telbivudine (Tyzekal)

ROUTE AND DOSAGE:
A: PO 600 MG/D

USES AND CONTRADICTIONS:
FOR CHRONIC HBV, PREGNANCY CATEGORY: B; PB 3.3%, t1/2 40 TO 49 H

8

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

adefovir dipivoxil (Hepsera)

ROUTE AND DOSAGE:
A/C > 12 Y: PO 10 MG/D

USES AND CONSIDERATION:
FOR CHRONIC HBV. PREGNANCY CATEGORY: C; PB: <4%; t1/2 7.4 H

9

NON-HIV ANTIVIRALS (SYSTEMIC/NONCLASSIFIED ANTIVIRALS):

entecavir (Baraclude)

ROUTE AND DOSAGE:
A: PO 0.5 TO 1 MG/D

USES AND CONSIDERATIONS:
FOR CHRONIC HBV. PREGNANCY CATEGORY: C; PB: 13%; t1/2 128 TO 149 H

10

NON-HIV ANTIVIRALS (SYSTEMIC/PURINE NUCLEOSIDES):

famciclovir (Famvir)

ROUTE AND DOSAGE:
HERPES ZOSTER: A: PO 500 MG Q8H x 7 D
HERPES SIMPLEX: A: PO 500 MG b.i.d. x 7 D

USES AND CONSIDERATIONS:
FOR HERPES ZOSTER AND HSV-1. PREGNANCY CATEGORY: B; PB: 20% TO 25%; t1/2 2 TO 3 H

11

NON-HIV ANTIVIRALS (SYSTEMIC/PURINE NUCLEOSIDES):

ganciclovir sodium (Cytovene)

USES AND CONSIDERATION:
A/C: IV: INITIALLY 5 MG/KG OVER 1 H x 7 D OR 6 MG/KG/D OVER 1 H x 5 D
maint: 5 MG/KG/D OVER 1 H x 7 D OR 6 MG/KG/D OVER 1 H x 5 D

USES AND CONSIDERATION:
FOR CMV SYSTEMIC INFECTION IN IMMUNOCOMPROMISED CLIENTS. PREGNANCY CATEGORY: C; PB 1% TO 2%; t1/2 2.5 TO 6 H

12

NON-HIV ANTIVIRALS (SYSTEMIC/PURINE NUCLEOSIDES):

ribavirin (Virazole)

1ST MARKETED IN 1986. ALSO USED FOR RESPIRATORY INFECTIONS CAUSED BY INFLUENZA A AND B VIRUSES IN OLDER ADULTS.
ROUTE AND DOSAGE:
RSV: C: AEROSOL INHALATION: 20 MG OVER 12 TO 18 H/D FOR 3 TO 7 D.
HEPATITIS C: A: >75 KG: PO 600 MG b.i.d. FOR 24 TO 48 WEEKS.
A: <75 KG: PO 400 MG IN MORNING AND 600 MG IN EVENING.
C: PO 15 MG/KG/D

USES AND CONSIDERATIONS:
FOR RESPIRATORY SYNCYTIAL VIRAL INFECTION (RSV) IN INFANTS AND CHILDREN AND HEPATITIS C. PREGNANCY CATEGORY: X; PB: NA; t1/2 24 H

13

NON-HIV ANTIVIRALS (SYSTEMIC/PURINE NUCLEOSIDES):

valacyclovir HCl (Valtrex)

ROUTE AND DOSAGE:
HERPES ZOSTER: A: PO 1 G t.i.d x 7 D
RECURRENT GENITAL HERPES: A: PO 500 MG b.i.d x 3 DAYS.

USES AND CONSIDERATIONS:
EFFECTIVE AGAINST VZV CAUSING HERPES ZOSTER (SHINGLES) AND RECURRENT GENITAL HERPES. MONITOR KIDNEY FUNCTION. ENCOURAGE CLIENT TO INCREASE WATER INTAKE. GI DISTURBANCES AND HEADACHES ARE COMMON SIDE EFFECTS. PREGNANCY CATEGORY: B; PB: 14% TO 18%; t1/2 2.5 TO 3.5 H

14

NON-HIV ANTIVIRALS (SYSTEMIC/PURINE NUCLEOSIDES):

valganciclovir (Valcyte)

PRODRUG OF GANCICLOVIR
ROUTE AND DOSAGE:
A: PO: 900 MG b.i.d WITH FOOD FOR 21 D

USES AND CONSIDERATIONS:
TO TREAT CMV-INFECTED CELLS OF RETINITIS IN AIDS CLIENTS. INHIBITS VIRAL DNA SYNTHESIS. MAY CAUSE LEUKOPENIA, THROMBOCYTOPENIA, BONE MARROW DEPRESSION, AND APLASTIC ANEMIA. PREGNANCY CATEGORY: C; PB: UK; t1/2 4 H

15

NON-HIV ANTIVIRALS (SYSTEMIC/NEURAMINIDASE INHIBITORS):

OSELTAMIVIR PHOSPHATE (Tamiflu)

ROUTE AND DOSAGE: A: PO 75 MG b.i.d X 50
C: <15 KG: PO 30 MG b.i.d x 5D
C: 15 TO 23 KG: PO 45 MG b.i.d x 5D
C: 23 TO 40 KG: PO 60 MG b.i.d x 5D
C: >40 KG: PO 75 MG b.i.d x 5D
A: INHALER: 2 ORAL INHALATIONS (ONE 5 MG BLISTER/INHALATION) b.i.d x 5D

USES AND CONSIDERATIONS: FOR UNCOMPLICATED ACUTE INFLUENZA A AND B. TREATMENT SHOULD BEGIN WITHIN 48 H OF 1ST FLU SYMPTOMS. MAY BE TAKEN WITH OR WITHOUT FOOD. SIDE EFFECTS INCLUDE TRANSIENT NAUSEA AND VOMITING. PREGNANCY CATEGORY: C; PB: 3%; t1/2 6 TO 10 H

16

NON-HIV ANTIVIRALS (SYSTEMIC/NEURAMINIDASE INHIBITORS):

zanamivir (Relenza)

ROUTE AND DOSAGE: A: INHALER: 2 ORAL INHALATIONS (ONE 5 MG BLISTER/INHALATION) b.i.d x 5D

USES AND CONSIDERATIONS:
FOR INFLUENZA A AND B AND H1N1 INFLUENZA. TREATMENT SHOULD BEGIN WITHIN 48 H OF 1ST FLU SYMPTOMS. LESS THAN 20% ABSORBED SYSTEMICALLY. PREGNANCY CATEGORY: C; PB: <10%; t1/2 2.5 TO 5 H

17

NON-HIV ANTIVIRALS (SYSTEMIC/TOPICAL NON-HIV ANTIVIRAL):

penciclovir (Denavir)

ROUTE AND DOSAGE:
A: TOPICAL: APPLY CREAM Q2H DURING THE DAY FOR 4 D.

USES AND CONSIDERATIONS:
FOR RECURRENT HERPES LABIALIS (COLD SORES) PREGNANCY CATEGORY: B; PB: UK; t1/2 UK

18

NON-HIV ANTIVIRALS (SYSTEMIC/TOPICAL NON-HIV ANTIVIRAL):

trifluridine (Viroptic)

ROUTE AND DOSAGE: A: OPHTHALMIC SOLUTION: 1 gt Q2H DURING THE DAY; MAX: 9 GTT/D

USES AND CONSIDERATIONS:
USED PRIMARILY FOR KERATOCONJUNCTIVITIS DUE TO HERPES SIMPLEX VIRUS. PREGNANCY CATEGORY: C; PB: UK; t1/2 12 MINUTES

19

VIRUSES:

MORE DIFFICULT TO ERADICATE THAN MOST TYPES OF BACTERIA. A VIRUS IS AN OBLIGATE INTRACELLULAR ORGANISM THAT USES THE CELL TO REPRODUCE. ENTERS HEALTHY CELLS AND USES DNA AND RNA TO GENERATE MORE VIRUSES.

20

THE GROWTH CYCLE OF VIRUSES DEPENDS ON?

THE HOST CELL ENZYME AND CELL SUBSTRATES FOR VIRAL REPLICATION. VIRUSES LIVE AND REPRODUCE WHEN THEY ARE WITHIN LIVING CELLS.

21

INFLUENZA

THE FLU; HIGHLY CONTAGIOUS VIRAL INFECTION; AFFECTS NOSE, THROAT, AND LUNGS. SEASONAL AND PREVALENT FROM DECEMBER TO MARCH. HAS 3 ANTIGEN TYPES: A, B, AND C.

22

INFLUENZA A

CAUSES MODERATE TO SEVERE INFECTION

23

INFLUENZA B

USUALLY CAUSES MILD ILLNESS IN CHILDREN

24

INFLUENZA C

VERY RARE IN HUMANS

25

INFLUENZA IS TRANSMITTED VIA?

CONTAMINATED DROPLETS DURING COUGHING, SNEEZING, OR TALKING. DROPLETS ENTER RESPIRATORY TRACT AND BEGINS REPLICATION 24 HOURS PRIOR TO APPEARANCE OF SYMPTOM.

26

SYMPTOMS OF INFLUENZA ARE?

THE FIRST IS A FEVER RISING TO 104 DEGREES F. THEN SORE THROAT, NONPRODUCTIVE COUGH, HEADACHE, CHILLS, PHOTOPHOBIA, AND MYALGIA MAY ALSO APPEAR.

27

FLU SHOT

CREATED FROM VIRUSES FROM THE PREVIOUS YEAR BECAUSE VIRUS CHANGES ITS STRUCTURE EACH YEAR. FOLLOWING VACCINE MOST INDIVIDUALS DEVELOP HIGH ANTIBODY TIER LEVELS PROVIDING PROTECTION AGAINST SIMILAR CIRCULATING VIRAL STRAINS. *EGGS ARE USED TO PRODUCE VACCINE, ALLERGIES TO EGGS MUST BE DETERMINED BEFORE THE VACCINE IS GIVEN.

28

FLU SHOT SUCCESS RATES

IN HEALTHY CHILDREN AND ADULTS 65% TO 90%;
OLDER ADULTS: 60% OF THE TIME, LESS THEN 60% IF AN AN OLDER ADULT HAS MULTIPLE HEALTH PROBLEMS.

29

HERPES VIRUSES ARE LARGE VIRUSES THAT CAUSE INFECTIONS. THE MOST FAMILIAR ARE:

1. HERPES SIMPLEX VIRUS TYPE 1 (HSV-1)
2. HSV-2
3. VARICELLA-ZOSTER VIRUSES (HSV-3 *CHICKENPOX/SHINGLES)
4. EPSTEIN-BARR VIRUS (HSV-4)
5. CYTOMEGALOVIRUS (HHV-5 *COMMONLY KNOWN AS CMV)

30

HSV-1:

ASSOCIATED WITH COLD SORES THAT GROW IN NEURONS; HAS ABILITY TO MAINTAIN DISEASE POTENTIAL WITHOUT SIGNS AND SYMPTOMS. CAPABLE OF CAUSING RECURRENT INFECTIONS; CAN REPLICATE IN MUCOUS MEMBRANES AND SKIN OF THE OROPHARYNX OR GENITALIA. VIRUS IS TRANSMITTED BY CONTACT WITH INFECTIOUS LESIONS OR SECRETIONS. SPREAD BY ORAL SECRETIONS FRON ONE INDIVIDUAL TO ANOTHER. FROM THE MOUTH,VIRUS CAN SPREAD TO GENITAL AREA BY ORAL INTERCOURSE OR POOR HAND WASHING.

31

HSV-2:

ASSOCIATED WITH GENITAL HERPES; REMAINS DORMANT BY TRAVELING THROUGH PERIPHERAL NERVES TO THE SACRAL DORSAL ROOT GANGLIA. CAN BE TRANSPORTED BACK TO THE NERVE ROOT TO EH SKIN FOR REACTIVATION AT ANY TIME. WHILE DORMANT VIRUS CONTINUES TO REPLICATE. CAPABLE OF CAUSING RECURRENT INFECTIONS; CAN REPLICATE IN MUCOUS MEMBRANES AND SKIN OF THE OROPHARYNX OR GENITALIA. VIRUS IS TRANSMITTED BY CONTACT WITH INFECTIOUS LESIONS OR SECRETIONS. SPREAD BY INTIMATE SEXUAL CONTACT, OR AN INFECTED MOTHER CAN TRANSMIT THE VIRUS TO HER INFANT DURING CHILDBIRTH.

32

SIGNS AND SYMPTOMS OF HSV-1 AND HSV-2

ERUPTION OF SMALL PUSTULES AND VESICLES; FEVER; HEADACHE; MALAISE; MYALGIA; AS WELL AS TINGLING, ITCHING, AND PAIN IN THE GENITAL AREA.

33

CYTOMEGALOVIRUS (CMV OR HHV-5)

VERY COMMON INFECTIOUS DISEASE WORLDWIDE; MOST ADULTS HAVE HAD IT BUT DIDNT EVEN KNOW. MOST PEOPLE DONT REQUIRE TREATMENT UNLESS THEY ARE IMMUNOCOMPROMISED (E.G. BABIES OR INDIVIDUALS WHO HAVE HAD ORGAN TRANSPLANTATION'S). TRANSMITTED VIA BODY FLUIDS. ESPECIALLY SALIVA OR URINE; KISSING, SEXUAL CONTACT, OR SHARING FOOD; OR BY PREGNANT WOMEN TO THEIR FETUS. CMV INFECTION CAN LEAT TO FATAL PNEUMONIA OR BLINDNESS (DUE TO AN INFECTED RETINA).

34

HEPATITIS B (HBV)

SERIOUS LIVER INFECTION CAUSED BY HEPATITIS B VIRUS; TRANSMITTED VIA NEEDLE-STICK, INTIMATE SEXUAL CONTACT, OR DURING CHILDBIRTH. HBV IS FOUND IN ALL BODY FLUIDS. SIGNS AND SYMPTOMS INCLUDE ANOREXIA, VOMITING, DIARRHEA, MUSCULAR PAIN, FATIGUE, AND COUGH.

35

DIAGNOSTIC TESTS FOR INFLUENZA

1. DIRECTION FLU A: HAS BEEN AVAILABLE FOR MANY YEARS TO DETECT INFLUENZA A; DOES NOT DETECT INFLUENZA B.
2. FLU OIA (THERMO BIOSTAR, BOULDER, CA), QUICKVUE INFLUENZA TEST (QUIDEL, SAN DIEGO), AND ZSTATFLU (ZYMETX, OK. CITY) NEW DIAGNOSTIC TESTS THAT IDENTIFY BOTH INFLUENZA A AND B. BY THROAT SWABS, NASAL SWABS, OR NASAL ASPIRATION. RESULTS AVAILABLE WITHIN 10 TO 20 MINUTES. QUICKVUE EASY AND FAST DIAGNOSIS OF INFLUENZA A AND B.

36

ANTIVIRAL DRUGS

USED TO PREVENT OR DELAY THE SPREAD OF A VIRAL INFECTION. INHIBIT VIRAL REPLICATION BY INTERFERING WITH VIRAL NUCLEIC ACID SYNTHESIS IN THE CELL.

37

INTERFERON ALFA-2A AND 2B ARE USED

TO TREAT HEPATITIS B AND C VIRUSES.

38

GAMMA GLOBULIN (IgG)

IS RICH IN ANTIBODIES FOUND IN THE BLOOD. PROVIDES A PASSIVE FORM OF IMMUNITY TO A VIRUS BY BLOCKING PENETRATION OF A VIRUS INTO THE HOST CELL. ADMINISTERED DURING EARLY INFECTIOUS STAGE OF AN ILLNESS TO PREVENT A VIRAL INVASION IN THE BODY.

39

HUMAN IMMUNE GLOBULIN (GAMASTAN):

ADMINISTERED: (IM) SINGLE-DOSE INJECTION PROTECTS FOR 2 TO 3 WEEKS; CAN BE REPEATED IN 2 TO 3 WEEKS. FOR CLIENTS WHO NEED AN IMMEDIATE INCREASE IN IMMUNE GLOBULIN LEVELS, (IV) IMMUNE GLOBULIN (GAMIMUNE N) MAY BE ADMINISTERED.

40

PURINE NUCLEOSIDES

EFFECTIVE IN INTERFERING WITH THE STEPS OF VIRAL NUCLEIC ACID (DNA) SYNTHESIS.

41

ACYCLOVIR SODIUM (ZOVIRAX)

DRUG CLASS AND DOSAGE:

DRUG CLASS: ANTIVIRAL; PREGNANCY CATEGORY: B

DOSAGE: HERPES SIMPLEX VIRUS:
A: PO 400 MG t.i.d FOR 7 TO 10 D
A: IV 5 TO 10 MG/KG Q8H FOR 10 TO 21 D
HERPES ZOSTER VIRUS:
A: PO 800 MG Q4H 5 x D FOR 7 TO 10 D
A/C: >12 Y: IV 10 MG/KG Q8H FOR 7 D
HERPES SIMPLEX ENCEPHALITIS:
A: IV 10 MG/KG Q8H x 10 D

42

ACYCLOVIR SODIUM (ZOVIRAX)

CONTRADICTIONS AND DRUG-LABEL-FOOD INTERACTIONS:

CONTRADICTIONS: HYPERSENSITIVITY, SEVERE RENAL OR HEPATIC DISEASE
CAUTION: ELECTROLYTE IMBALANCE, NURSING MOTHERS, YOUNG CHILDREN.

DRUG-LABEL-FOOD INTERACTIONS:
DRUG- INCREASE NEPHRO-NEUROTOXICITY WITH AMINOGLYCOSIDES, PROBENECID, INTERFERON.
LAB: MAY INCREASE AST, ALT, BUN

43

ACYCLOVIR SODIUM (ZOVIRAX)

PHARMACOKINETICS AND PHARMACODYNAMICS:

PHARMACOKINETICS:
ABSORPTION: PO SLOWLY ABSORBED
DISTRIBUTION: PB 10% TO 30%
METABOLISM: t1/2 PO 2 TO 3 H
EXCRETION: URINE AND BREAST MILK
PHARMACODYNAMICS: PO: ONSET UK
PEAK: 1.5 TO 2 H
DURATION: 4 TO 8 H
IV: ONSET RAPID
PEAK: 1 TO 2 H
DURATION: 4 TO 8 H

44

ACYCLOVIR SODIUM (ZOVIRAX)

THERAPEUTIC EFFECTS/USES, SIDE EFFECTS, AND ADVERSE REACTIONS:

THERAPEUTIC EFFECTS/USES: TO TREAT HSV-1 AND HSV-2 (GENITAL), HERPES ZOSTER (SHINGLES) & CMV
MODE OF ACTION: INTERFERENCE WITH VIRAL SYNTHESIS OF DNA.
SIDE EFFECTS: NAUSEA, VOMITING, DIARRHEA, HEADACHE, TREMORS, LETHARGY, RASH, PRURITUS, INCREASED BLEEDING TIME, PHLEBITIS AT IV SITE
ADVERSE REACTIONS: URTICARIA, ANEMIA, GINGIVAL HYPERPLASIA
LIFE-THREATENING: NEUROPATHY, SEIZURES, NEPHROTOXICITY (LARGE DOSES), BONE MARROW DEPRESSION, THROMBOCYTOPENIA, LEUKOPENIA, GRANULOCYTOPENIA

45

ACYCLOVIR SODIUM (ZOVIRAX) MORE INFORMATION:

RESISTANCE: RESULT OF LACK OF VIRAL-PRODUCING ENZYME (THYMIDE KINASE) NEEDED TO CONVERT THE DRUG TO AN EFFECTIVE ANTIVIRAL COMPOUND.
PHARMOKINETICS: HALF THE DRUG PASSES INTO THE CEREBROSPINAL FLUID. EXCRETED UNCHANGED IN URINE. (EXCRETED IN BREAST MILK TOO)
PHARMACODYNAMICS: PROBENECID CAN INCREASE THE EFFECTS OF ACYCLOVIR. IF AN AMINOGLYCOSIDE OR AMPHOTERICIN B IS TAKEN WITH ACYCLOVIR, THE INCIDENCE OF NEPHROTOXITY IS INCREASED.

46

VALACYCLOVIR (VALTREX)

CONVERTED TO ACYCLOVIR; WITH HERPES ZOSTER, IT OFFERS A GREATER DECREASE IN PAIN AND AN INCREASE IN HEALING TIME (40 TO 43 DAYS) WITH ACYCLOVIR (59 DAYS).

47

FAMCICLOVIR (FAMVIR)

AN ANTIVIRAL DRUG DEVELOPED BEFORE VALACYCLOVIR, IS EQUALLY EFFECTIVE AS ACYCLOVIR FOR TREATING ACUTE HERPES ZOSTER.

48

GANCICLOVIR

CAN CAUSE THROMBOCYTOPENIA AND GRANULOCYTOPENIA. BECAUSE OF POSSIBLE SERIOUS ADVERSE REACTIONS, THIS DRUG SHOULD BE PRESCRIBED PRIMARILY FOR SEVERE SYSTEMIC CMV INFECTIONS FOR IMMUNOCOMPROMISED CLIENTS.

49

ANTIVIRAL HIV DRUGS

HIV IS A RETROVIRUS. THERE ARE TWO CLASSES OF ANTIRETROVIRAL DRUGS (1) REVERSE TRANSCRIPTASE INHIBITORS AND (2) PROTEASE INHIBITORS. ANTIVIRAL DRUGS CLASSIFIED AS REVERSE TRANSCRIPTASE INHIBITORS INCLUDE: delavirdine (Rescriptor), didanosine (Videx), Iamivudine (Epivir), nevirapine (Viramune), stavudine (Zerit), and zidovudine (Retrovir, AZT). THEY AID IN INHIBITING VIRAL REPLICATION.

50

Zidovudine

FIRST RETROVIRAL DRUGS PASSED BY FDA. IT INHIBITS THE ACTION OF VIRAL REVERSE TRANSCRIPTASE, THUS PREVENTING THE SYNTHESIS OF DNA AND ALLOWING THE T3 LYMPHOCYTES TO INCREASE INITIALLY.

51

PROTEASE INHIBITOR GROUP INCLUDE:

indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), and saquinavir (Invirase). this group inhibits the replication of retroviruses (HIV-1 and HIV-2). when used in combination with reverse transcriptase inhibitor, these drugs may greatly reduce the viral level to the point that it is undetectable. Combination of drugs helps decrease HIV drug resistance.

52

ANTIMALARIALS:

hydroxychloroquine sulfate (Plaquenil sulfate)

ROUTE AND DOSAGE: ACUTE MALARIA:
A: PO 620 MG BASE OR 800 MG, THEN 310 MG BASE OR 400 MG AT 6, 18, AND 24 H.
C: PO 10 MG BASE/KG/DOSE, 6 H: 5 MG BASE/KG; 5 MG BASE/KG/D FOR 2 D.

USES AND CONTRADICTIONS:
ALTERNATIVE TO CHLOROQHINE. DOSAGE VARIES FOR TREATING MALARIA. CAN BE USED ADJUNCTIVELY WITH PRIMAQUINE. GIVE DRUG WITH MEALS TO REDUCE OCCURANCE OF GI DISTRESS. PREGNANCY CATEGORY: C; PB: 45%; t1/2 70 TO 120 H.

53

ANTIMALARIALS:

mefloqhine HCI (Lariam)

ROUTE AND DOSAGE: MALARIA TREATMENT:
A: PO SINGLE DOSE: 1250 MG
MALARIA PROPHYLAXIS:
A: PO 250 MG Q WK x 4 WK; TAKE WITH PLENTY OF WATER.

USES AND CONSIDERATIONS:
PROPHYLAXIS AND TREATMENT OF ACUTE MALARIA. PREGNANCY CATEGORY: C; PB: 98%; t1/2 10 TO 21 D
ADVERSE EFFECTS: SEVERE ANXIETY, RESTLESSNESS, DISORIENTATION, DEPRESSION, HALLUCINATIONS, PARANOIA, AND SUICIDAL THOUGHTS.

54

ANTIMALARIALS:

primaquine phosphate (Primaquine)

ROUTE AND DOSAGE:
MALARIA PROPHYLAXIS: A: PO 15 MG/D FOR 14 D.
MALARIA TREATMENT: A: PO 30 MG/D FOR 14 D.

USES AND CONSIDERATIONS:
FOR CERTAIN PLASMODIUM SPP. (P. vivax AND P. ovale) AND PNEUMOCYSTIS carini PNEUMONIA. CAN AFFECT WBC PRODUCTION (GRANULOCYTOPENIA) AND CAUSE ACUTE HEMOLYTIC ANEMIA IN CLIENTS WITH G-6-PD DEFICIENCY. PREGNANCY CATEGORY: C; PB: UK; t1/2 3.7 TO 9.6 H

55

ANTIMALARIALS:

pyrimethamine (Daraprim)

ROUTE AND DOSAGE: MALARIA PROPHYLAXIS:
A/C: >10 Y; PO 25 MG/WK
C: <4 Y: PO 6.25 MG/WK
C: 4 TO 10 Y: PO 12.5 MG/WK

USES AND CONSIDERATIONS: PROPHYLAXIS USED FOR MALARIA. FOR CHLOROQUINE RESISTANT Plasmodium falciparum INFECTIONS. MAY BE USED WITH QUINACRINE, QUININE, OR CHLOROQUINE. PREGNANCY CATEGORY: C; PB: 80%; t1/2 54 TO 148 H

56

ANTIMALARIALS:

quinine sulfate (Novoquinine)

ROUTE AND DOSAGE:
ACUTE MALARIA: A: PO 650 MG Q8H FOR 3 TO 7 D

USES AND CONSIDERATIONS: USED IN COMBINATION DRUG THERAPY OR FOR CHLOROQUINE-RESISTANT MALARIA. USED TO TREAT NOCTURNAL LEG CRAMP. PREGNANCY CATEGORY: C; PB: 70%; t1/2 6 TO 14 H

57

COMBINATION ANTIMALARIAL DRUGS:

atovaquone/proguanil (Malarone)

ROUTE AND DOSAGE: A/C: >40 KG; PO 250/100 MG FOR 1 TO 2 D. PRIOR TO VISITING MALARIAL AREA, DURING STAY, AND FOR 7 DAYS AFTER LEAVING AREA.
C: <40 KG: 62.5/25 TO 187.5/75 MG/D PRIOR TO VISITING MALARIAL AREA, DURING STAY, AND FOR 7 DAYS AFTER LEAVING AREA.

USES AND CONSIDERATIONS: FOR ORAL PROPHYLAXIS AND TREATMENT OF MALARIA. EFFECTIVE FOR CHLOROQUINE-RESISTANT STRAINS. PREGNANCY CATEGORY: C; PB: 99%; t1/2 2 TO 3 D/12 TO 20 H

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COMBINATION ANTIMALARIAL DRUGS:

artemether/lumefantrine (Coartem)

ROUTE AND DOSAGE:
A/C: >35 KG: PO 4 TABLETS OF ARTEMETHER 80 MG/LUMEFANTRINE 480 MG UPON DIAGNOSIS THEN 4 TABLETS IN 8 H, THEN 4 TABLETS MORNING AND EVENING FOR 2 D.
A/C: 25 TO 35 KG: PO 3 TABLETS IN SAME REGIMEN.
C: 15 TO 25 KG; PO 2 TABLETS IN SAME REGIMEN.
C: 5 TO 15 KG: PO 1 TABLET IN SAME REGIMEN.

USES AND CONSIDERATIONS: FOR MALARIA INFECTIONS THAT ARE BOTH DRUG-SENSITIVE AND DRUG-RESISTANCE TO Plasmodium falciparum. ACTS BY INHIBITING NUCLEIC ACID AND PROTEIN SYNTHESIS. THE RAPID ONSET ALLOWS THE DRUG TO CONTROL FEVER QUICKLY. WAS FDA APPROVED IN APRIL, 2009 AND HAS HAD A HIGH CURE RATE. ADVERSE EFFECTS INCLUDE NYSTAGMUS, WHEEZING, HYPOKALEMIA, BLOOD DYSCRASIAS, AND HEPATOMEGALY. PREGNANCY CATEGORY: C; PB: 95%/99%; t1/2 2 TO 3 H/3 TO 6 D.

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MALARIA IS CAUSED BY?

PROTOZOAN PARASITES Plasmodium spp. CARRIED BY INFECTED Anopheles MOSQUITOES AND IS ONE OF THE MOST PREVALENT PROTOZOAN DISEASES.

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PROTOZOAN PARASITE PASSES THROUGH TWO PHASES:

1. TISSUE PHASE: INVASION OF BODY TISSUE; PRODUCES NO CLINICAL SYMPTOMS IN THE HUMAN.
2. ERYTHROCYTIC PHASE: INVASION OF THE RED BLOOD CELLS; CAUSES SYMPTOMS OF CHILLS, FEVER, AND SWEATING.
INCUBATION PERIOD IS 10 TO 35 DAYS, FOLLOWED BY FLU-LIKE SYMPTOMS.

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THERE ARE 50 SPECIES OF Plasmodium, 4 TYPES OF THE SPECIES CAUSE MALARIA THEY ARE?

P. malariae, P. ovale, P. vivax and P. falciparum.

*P. vivax most prevalent.
*P. falciparum most severe.

PRIMARY CAUSES IS BECAUSE OF TRAVEL TO REGIONS IN THE WORLD WHERE MALARIA IS ENDEMIC, AND DRUG-RESISTANT MALARIA PARASITES.

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TREATMENT OF MALARIA DEPENDS ON ?

TYPE OF Plasmodium AND THE ORGANISMS LIFE CYCLE.

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CHLOROQUINE AND HYDROXY-CHLOROQUINE

CAN BE TOXIC TO CHILDREN AND MAY EVEN CAUSE DEATH; THEREFORE THE DRUG DOSE SHOULD BE CLOSELY MONITORED.

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THREE METHODS USED TO ERADICATE MALARIA ARE ?

1. PROPHYLAXIS (PREVENTION) OF MALARIA
2. TREATMENT FOR THE ACUTE ATTACK
3. PREVENTION OF RELAPSE

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PREVENTING MEDICATION ERRORS

DO NOT CONFUSE: QUININE (ANTIMALARIAL) WITH QUINIDINE (ANTIDYSRHYTHMIC). THEY LOOK ALIKE, BUT THE ACTIONS AND PHARMACOLOGY ARE VERY DIFFERENT.

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Chloroquine HCL:

DRUG CLASS:

ANTIMALARIAL
TRADE NAME: Aralen HCL
PREGNANCY CATEGORY: C

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Chloroquine HCL:

DOSAGE:

ACUTE MALARIA:
A: PO 600 MG BASE/DOSE; THEN IN 6 H; 300 MG/DOSE; THEN AT 24 AND 48 H: 300 MG FOR 2 D.
A: IM 200 MG/BASE Q6H, PRN;
C: PO 10 MG BASE/KG/DOSE, THEN 5 BASE/KG IN 6 H, 24 H, AND 36 H AFTER FIRST DOSE.
C: IM 5 MG BASE/KG, REPEAT IN 6 H PROPHYLAXIS. 2 WK BEFORE AND FOR 6 TO 8 WK AFTER EXPOSURE.
A: PO 300 MG BASE WKLY
C: PO 5 MG/KG/WK;

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Chloroquine HCL:

CONTRAINDICTIONS AND DRUG-LABEL FOOD INTERACTIONS:

CONTRAINDICTIONS: HYPERSENSITIVITY TO 4-AMINOQUINOLONES; RENAL DISEASE, PSORIASIS, RETINAL CHANGES.
CAUTION: ALCOHOLISM; LIVER DYSFUNCTION; G-6-PD DEFICIENCY; GI NEUROLOGIC, AND HEMATOLOGIC DISORDERS.

DRUG-LABEL FOOD INTERACTIONS:
DRUG: INCREASE EFFECTS OF DIGOXIN, ANTICOAGULANTS, NEUROMUSCULAR BLOCKER; DECREASE ABSORPTION WITH ANTACIDS AND LAXATIVES
LAB: DECREASE RED BLOOD CELL COUNT, HEMAGLOBIN, HEMATOCRIT.

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Chloroquine HCL:

PHARMACOKINETICS AND PHARMACODYNAMICS:

PHARMACOKINESTICS: ABSPORTION- WELL ABSORBED FROM GI TRACT. INHIBITS THE MALARIA PARASITE'S GROWTH BY INTERFERING WITH ITS PROTEIN SYNTHESIS. DISTRUCTION- PB 50% TO 65%.
METABOLISM- t1/2 1.5 TO 2 D
EXCRETION: EXCRETED SLOWLY IN URINE.

PHARMACODYNAMICS:
PO: ONSET: RAPID; PEAK: 3.5 H; DURATION: DAYS TO WEEKS.
IM: ONSET: RAPID; PEAK: 0.5 H; DURATION: DAYS TO WEEKS.

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Chloroquine HCL:

THERAPEUTIC EFFECTS/USES, SIDE EFFECTS, ADVERSE REACTIONS:

THERAPEUTIC EFFECTS/USES: TO TREAT ACUTE MALARIA; PROPHYLAXIS FOR MALARIA.
MODE OF ACTION: INCREASED pH IN THE MALARIA PARASITE INHIBITS PARASITIC GROWTH.
SIDE EFFECTS: ANOREXIA, NAUSEA, VOMITTING, DIARRHEA, ABDOMINAL CRAMPS, FATIGUE, PRURITUS, NERVOUSNESS, VISUAL DISTURBANCES (BLURRED VISION)
ADVERSE REACTIONS: ECG CHANGES, HYPOTENSION, PSYCHOSIS, LIFE-THREATENING, AGRANULOCYTOSIS, APLASTIC ANEMIA, THROMBOCYTOPENIA, OTOTOXITY, CARDIOVASCULAR COLLAPSE.

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ANTIMALARIAL DRUGS:

DRINK PLENTY OF FLUIDS, IS A COMBO TREATMENT, TAKE WITH A FULL STOMACH.

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HELMINTHS

ARE LARGE ORGANISMS (PARASITE WORMS) THAT FEED ON HOST TISSUE. MOST COMMON SITE OF HELMINTHIASIS (WORM INFESTATION) IS THE INTESTINE. OTHER SITES ARE: LYMPHATIC SYSTEM, BLOOD VESSELS, AND LIVER.

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THERE ARE 4 GROUPS OF HELMINTHS:

1. CESTODES (TAPEWORMS)
2. TREMATODES (FLUKES)
3. INTESTINAL NEMATODES (ROUNDWORMS)
4. TISSUE-INVADING NEMATODES (TISSUE ROUNDWORMS AND FILARIAE)

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CESTODES (TAPEWORMS)

SEGMENTED AND ENTER THE INTESTINE VIA CONTAMINATED FOOD. THERE ARE FOUR SPECIES OF THEM:
1. Taenia solium (Pork Tapeworm)
2. Taenia saginata (Beef Tapeworm)
3. Diphyllobothrium latum (Fish Tapeworm)
4. Hymenolepis nana (dwarf tapeworm)
Segmented cestodes have heads and hooks or suckers that attach to the tissue.

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TREMATODES (FLUKES)

ARE FLAT, NON-SEGMENTED PARASITES THAT FEED ON THE HOST. THERE ARE FOUR TYPES:
1. Fasciola hepatica (liver fluke)
2. Fasciolopsis buski (intestinal fluke)
3. Paragonimus westermani (lung fluke)
4. Schistosoma species (blood fluke)

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INTESTINAL NEMATODES

MAY FEED ON INTESTINAL TISSUE;
1. Ascaris lumbricoides (Giant Roundworm)
2. Necator americanus (Hookworm)
3. Enterobius vermicularis (Pinworm)
4. Strongyloids stercoralis (Threadworm)
5. Trichuris trichiura (Whipworm)

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TISSUE-INVADING NEMATODES:

1. Trichinella spiralis (Pork Roundworm)
2. Wuchereria bancrofti (filariae)

PORK ROUNDWORM OR T. spiralis, CAN CAUSE TRICHINOSIS (DISEASE CAUSED BY INGESTION OF RAW OR INADEQUATELY COOKED PORK THAT CONTAINS LARVAE OF THE T. spiralis PARASITE).
CAN BE DIAGNOSED BY A MUSCLE BIOPSY.
THOROUGHLY COOKING PORK, THE ROUNDWORM, IF PRESENT, IS DESTROYED.

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ANTHELMINTIC DRUGS:

bithionol (Actamer)

ROUTE AND DOSAGE: UK

USES AND CONSIDERATIONS: EFFECTIVE AGAINST FLUKES. FOR Paragonimus westermani (lung fluke)

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ANTHELMINTIC DRUGS:

diethylcarbamazine (Hetrazan)

ROUTE AND DOSAGE: A: PO 2 TO 3 MG/KG t.i.d

USES AND CONSIDERATIONS: FOR nematode-filariae

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ANTHELMINTIC DRUGS:

ivermectin (Stromectol)

ROUTE AND DOSAGE:
A/C: >15 KG: PO 200 MG/KG, SINGLE DOSE

USES AND CONSIDERATIONS: A BROAD SPECTRUM ANTIPARASITIC DRUG. CAUSES PARALYSIS TO THE PARASITE HIGHLY ACTIVE AGAINST VARIOUS MITES. PREGNANCY CATEGORY: C; PB: UK; t1/2 16 H

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ANTHELMINTIC DRUGS:

mebendazole (Vermox)

ROUTE AND DOSAGE:
A/C: PO 100 MG q.d. TO b.i.d x 3 D

USES AND CONSIDERATIONS: FOR GIANT ROUNDWORM, HOOKWORM, PINWORM, WHIPWORM
PREGNANCY CATEGORY: C; PB: UK; t1/2 3 TO 9 H

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ANTHELMINTIC DRUGS:

piperazine citrate (Entacyl)

ROUTE AND DOSAGE:
ROUNDWORM: A: PO 3.5 g/d x 2 d; REPEAT IN ONE WEEK PRN.
C: PO 75 MG/KG/D x 2 D; MAX: 3.5 G/D; REPEAT IN ONE WEEK PRN.
PINWORMS: A/C: 65 MG/KG/D x 7 D; MAX: 2.5 G/D
USES AND CONSIDERATIONS: FOR ROUNDWOMRS AND PINWORMS. PREGNANCY CATEGORY: B; PB: UK; t1/2: UK

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ANTHELMINTIC DRUGS:

praziquantel (Biltricide)

ROUTE AND DOSAGE:
A/C: >4 Y: PO 20 TO 25 MG/KG t.i.d x 1 TO 2 D

USES AND CONSIDERATIONS: FOR BEEF, PORK, AND FISH TAPEWORMS, BLOOD FLUIDS; AND LIVER, LUNG, AND INTESTINAL FLUKES. PREGNANCY CATEGORY: B; PB: 80% TO 85%; t1/2: 0.8 TO 1.5 H

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ANTHELMINTIC DRUGS:

pyrantel pamoate (Pin-X)

ROUTE AND DOSAGE:
A/C: >2 Y: PO 11 MG/KG; SINGLE DOSE; MAX: 1 G

USES AND CONSIDERATIONS: FOR GIANT ROUNDWORM, HOOKWORM, AND PINWORM. PREGNANCY CATEGORY: C; PB: UK; t1/2: UK

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ANTHELMINTIC DRUGS:

thiabendazole (Mintezol)

ROUTE AND DOSAGE:
A: <70 KG PO 1.5 G b.i.d FOR 2 TO 5 D
C: 57 TO 67 KG PO 1.25 G b.i.d
C: 46 TO 56 KG PO 1 G b.i.d
C: 14 to 45 KG PO 25 MG/KG b.i.d FOR 2 TO 5 D

USES AND CONSIDERATIONS: FOR THREAD-WORM AND PORK WORM. PREGNANCY CATEGORY: C; PB: UK; t1/2: 1 H

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SIDE EFFECTS OF ANTHELMINTICS (AGENTS THAT DESTROY WORMS)

*TAKE WITH FOOD, AND DO NOT DRIVE*

GI DISTRESS, WHICH CAN MANIFEST AS ANOREXIA, NAUSEA, VOMITING, AND OCCASIONALLY DIARRHEA AND STOMACH CRAMPS.

NEUROLOGIC PROBLEMS: DIZZINESS, WEAKNESS, HEADACHE, AND DROWSINESS.

THIABENDAZOLE SHOULD BE AVOIDED IF THE CLIENT HAS LIVER DISEASE.