ANTI-PROTOZOAL - SULFONAMIDES Flashcards
1
Q
- anaerobic, microaerophilic bacteria and protozoa
- “TRIAD OF FEATURES” which includes antiamebic, antigiardiasis, and antitrichomonal
A
METRONIDAZOLE
2
Q
DOC for AMOEBA, GIARDIASIS / LABIASIS, TRICHOMONAL
A
METRONIDAZOLE
3
Q
MOA:
* enters cell via CELL DIFFUSION
* NITROREDUCTION – similar with nitrofurans (produces FREE RADICALS)
* activated via single reduction step by bacteria → forms RADICALS → reacts with nucleic acid (by covalently binding the 5-nitro group to DNA) → cell death
A
METRONIDAZOLE
4
Q
METRONIDAZOLE:
responsible for its stability in IV and tablet form
A
ethanoic moiety
5
Q
- esters are to be ACTIVATED to exert amebicidal activity
- tx of asymptomatic carriers of E. histolytica
A
DILOXANIDE
6
Q
- antibacterial and antifungal
- parent compound
A
8-hydroxyquinoline
7
Q
- tx of ACUTE and CHRONIC INTESTINAL AMOEBIASIS
- AE: nueropathy
A
IODOQUINOL
8
Q
IODOQUINOL:
adverse effect
A
neuropathy
9
Q
- alkaloids obtained from IPECAC
- amoebicidal
- protoplasmic poison
- tx for LIVER disease since alkaloids concentrates mainly at the liver
- tx for BALANTIDIAL DYSENTERY and FLUKE infestations
A
EMETINE & DEHYDROEMETINE
10
Q
- tx of PNEUMONIA caused by P. carinii
- tx for the prophylaxis of AFRICAN TRYPANOSOMIASIS
- tx for VISCERAL LEISHMANIAISIS
A
PENTAMIDINE ISETHIONATE
11
Q
- highly RESISTANT to MALARIA
- highly LIPOPHILIC
- water INSOLUBLE analogue of ubiquinone 6
- tx of PCP caused by P. carinii (alternative)
- originally an antimalarial Plasmodium falciparum develops tolerance to its action
- high fat diet to improve absorption
A
ATOVAQUONE
12
Q
- inhibitor of ORNITHINE DECARBOXYLASE
- tx of West African SLEEPING SICKNESS caused by T. gambiense
A
EFLORNITHINE
13
Q
- NITROFURAN derivative
- tx of ACUTE and CHRONIC CHAGA’S disease (DOC)
A
NIFURTIMOX
14
Q
- NITROIMIDAZOLE derivative as an alternative in the treatment of CHAGA’S disease
- SE: peripheral neuropathy, bone marrow suppression
A
BENZNIDAZOLE
15
Q
BENZNIDAZOLE:
side effects
A
peripheral neuropathy
bone marrow supression
16
Q
- DOC for later stages OF AFRICAN TRYPANOSOMIASIS
- excellent PENETRATION into the CNS
- causes ARSENIC toxicity
A
MELARSOPROL
17
Q
MELARSOPROL:
adverse effect
A
arsenic toxicity
18
Q
- pentavalent ANTIMONY-compound intended primarily for the tx of various LEISHMANIASIS (DOC)
- LOW TI
- should be monitored for heavy metal
A
SODIUM STIBOGLUCONATE
19
Q
- HEAVY METAL POISON
- MOA: chelation
A
DIMERCAPROL
20
Q
DIMERCAPROL:
MOA
A
chelation
21
Q
- DOC for long term ____
- PROPHYLACTIC agent for AFRICAN TRYPANOSOMIASIS
A
SURAMIN SODIUM
22
Q
- alternative for the treatment of Ascaris lumbcricoides and Enterobius vermicularis
- anticholinergic
- tx for PINWORM and ROUNDWORM
A
PIPERAZINE
23
Q
PIPERAZINE MOA:
increase the ____ of the helminth muscle so that the muscle membrane is supressed leading to FLACCID PARALYSIS
A
resting potential
24
Q
- SELECTIVE anthelmentic activity against FILARIASIS and ASCARIASIS
A
DIETHYLCARBAMAZEPINE CITRATE
25
* tx of **PINWORMS** and **ASCARIS**
* **DEPOLARIZING NEUROMUSCULAR** blocking agent
* ANTAGONIZE **piperazine**
PYRANTEL PAMOATE
26
PYRANTEL PAMOATE:
**adverse effect**
GI effect
27
**PYRANTEL EMBONATE****MOA**:
promotes ____ of the **helminth's MYONERUAL JUNCTION** and ____ → **spastic paralysis** and **loss** of **muscle activity**
depolarization
cholinesterase inhibition
28
* **broad spectrum** anthelmintic activity in **human** and **livestock**
* relive symptoms associated with **CUTANEOUS LARVA MIGRANT** and **invasive phase** of **THRICOSIS**
THIABENDAZOLE
29
* broad spectrum anthelmintic activity similar with thiabendazole
* MOA: **inhibition** of **GLUCOSE UPTAKE** leading to **depleted glycogen storage** → decrease ATP synthesis
* AE: **abdominal discomfort** and **teratogenic**
MEBENDAZOLE
30
**MEBENDAZOLE MOA**:
inhibition of ____ leading to **depleted glycogen storage** → decrease ATP synthesis
glucose uptake
31
MEBENDAZOLE:
**adverse effects**
abdominal discomfort
teratogenic
32
* broad spectrum anthelmentic activity against **NEMATODES** (intestinal)
* **SINGLE-DOSE** tx for **ASCARIASIS**, **HOOKWORM**, and **TRICHURIASIS**
* **MULTIPLE DOSE** therapy wfor the tx of **PINWORM**, **THREADWORM**, **CAPILLARIASIS**, **CHLORNORCHIASIS**, and **HYDATID** disease
| **HYDATID** - seen in dogs
ALBENDAZOLE
33
ALBENDAZOLE:
____ for **ASCARIASIS**, **HOOKWORM**, and **TRICHURIASIS**
SINGLE DOSE
34
ALBENDAZOLE:
____ for the tx of **PINWORM**, **THREADWORM**, **CAPILLARIASIS**, **CHLORNORCHIASIS**, and **HYDATID** disease
MULTIPLE DOSE
35
* active against **BLOOD TREMATODE**: Shistosoma hematobium, S. japonicum, S. mansoni
* leads to **BLOODY STOOL**
NIRIDAZOLE
36
**NIRIDAZOLE MOA**:
inhibits the **CONVERSION** of the **active form** of ____ into **inactive form**
schistosomal glycogen phosphorylase
37
* **TAENICIDE**, a **saline purge** 1-2hrs after ingestion is recommended to **REMOVE** the **SCOLEX** and **WORM SEGMENTS**
* potent **TAENICIDE** that **segments** worms and scolex
NICLOSAMIDE
38
**NICLOSAMIDE MOA**:
inhibition of ____, ____ by **ANaerobic** metabolism and inhibition of ____ into **ATP**
inhibition of glucose uptake, energy production, inorganic phosphate incorporation
39
* **CHLORINATED BISPHENOL** formerly used in **soaps** and **cosmetics** for its antimicrobial activity
* **Fasciolicide** and **Taenicide**
BITHIONOL
40
* anti**schistosomial** agent for **INTESTINAL SCHISTOSOMIASIS**
OXAMNIQUINE
| OXAM sa HISTO
41
* broad spectrum against **FLUKES**
* DOC: **BLOOD FLUKES**
PRAZIQUANTEl
| ZI QUAN pang DUGO
42
**PRAZIQUANTEL MOA**:
produces ____ **contraction** within the **muscle system** of the fluke (**alteration** in the **influx** of **calcium ions**) leading to **segment worms**
TETANIC-LIKE
43
* obtained from **STREP. AVERMITILIS**
* used in controlling **ENDO** and **ECTO** parasites in **DOMESTIC ANIMALS**
* effective for **ONOCHOCERCIARIS** in **humans** that is caused by *Oncocerca volvulus*
IVERMECTIN
44
# **DOC: NEMATODES**
***Ascaris lumbricoides***
(**round**worm)
**PAM**
Pyrantel palmoate
Albendazole
Mebendazole
45
# **DOC: NEMATODES**
**HOOKWORM**
**PAM**
Pyrantel palmoate
Albendazole
Mebendazole
46
**OLD**-world hookworm
Anyclostoma duodenale
47
**NEW**-world hookworm
Necator americanus
48
# **DOC: NEMATODES**
**TRICHURIS**
*Trichuris trichuria*
**AM**
Albendazole
Mebendazole
48
# **DOC: NEMATODES**
**STRONGYLOIDES**
Ivermectin
| STRONG si IVER
49
# **DOC: NEMATODES**
***Enterobius vermivularis***
**PM**
Pyrantel palmoate
Mebendazole
| PM mo si VERMI
50
# **DOC: NEMATODES**
**TRICHINELLA**
Mebendazole
| ELLA & BEN
51
# **DOC: NEMATODES**
**CUTANEOUS LARVA MIGRANS**
**AI**
Albendazole
Ivermectin
| nag MIGRATE si AIAI
52
# **DOC: NEMATODES**
**ONCHOCERCA VOLVULUS**
Ivermectin
| ECHOSERA si IVER
53
# **DOC: TREMATODES**
Shistosoma ***haematobium***
Schistosoma ***mansoni***
Schistosoma ***japoniucm***
***Paragonimus westermani***
PRAZIQUANTEL
| nag SCHI (ski) at PARAgliding SI KWAN (ziquan)
54
# **DOC: TREMATODES**
***Fasciola hepatica***
**Bi**thionol
**Tri**clalbendazole
| may HEPA si no. 23
54
55
# **DOC: TREMATODES**
***Fasciolopsis buski***
Praziquantel
Niclosamide
| si AZI at NICO ay naglaro ng BUSKItbol
56
# **DOC: CESTODES**
Taenia ***saginata***
Taenia ***solium***
Praziquantel
Niclosamide
| kumain ng SAGing galing sa SOIL si AZI at NICO
57
# **DOC: CESTODES**
***Hymenolepsis nana***
Niclosamide
| kumain ng HYMEN si NICO
58
# **DOC: CESTODES**
***Cysticercosis***
Albendazole
| may CYST si ALBEN
59
# **DOC: CESTODES**
***Diphylobothrium latum***
Praziquantel
Niclosamide
| naglaro ng LATU LATU si AZI at NICO
60
# **DOC: CESTODES**
***Echinococcus granulosus***
Albendazole
| CHINO & ALBEN richards
61
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
compounds used to control **MITES** (***Sarcoptes scabiei***)
SCABICIDE
62
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
used to eliminate **head**, **body**, and **crab LICE**, **FLEAS**
PEDICULICIDE
63
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
* **ester** from **PERU BALSAM**
* **topical** scabicide
BENZOYL BENZOATE
64
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
BENZOYL BENZOATE:
**components**
benzyl alcohol
benzoyl chloride
65
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
* **HALOGENATED HYDROCARBON** with insecticidal activity
* a **DIRECT POISON**, **fumigant** effect, acts as a **STOMACH POISON**
* tx of **SCABIES** and **PEDICULOSIS**
LINDANE
66
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
**TOPICAL** tx of **SCABIES**
Crotamiton
67
# **ANTISCABIOUS AND ANTIPEDICULAR AGENTS**
* synthetic **PYRETHRINOID** compound
* derived from **permethrone**
* exerts **lethal action** against **LICE**, **TICKS**, **MITES**, and **FLEAS**
* **pediculicide** fofr the treatment of **HEADLICE**
PERMETHRIN
68
# **ANTIBACTERIAL SULFONAMIDES**
is **SULFONAMIDES** a **TMP** antibiotics?
| **TRIMETHOPRIN**
NO
sulfonamides are SYNTHETIC antibacterial agents
69
# **ANTIBACTERIAL SULFONAMIDES**
**PARENT compound** of SULFONAMIDES
PRONTOSIL
70
brilliant azo red dye
PRONTOSIL
71
**NATURAL products** biosynthesized by microorganisms that are **toxic** to toher species of microorganisms
ANTIBIOTICS
72
____ were the **FIRST SUCCESSFUL SELECTIVELY TOXIC** antibacterial drugs
SULFONAMIDES
73
# **SULFONAMIDES**
____ was discovered by **GERHARD DUGMAK** in **1936**
PRONTOSIL
74
# **SULFONAMIDES**
**PRONTOSIL** was discovered by ____
GERHARD DUGMAK, 1936
75
# **SULFONAMIDES**
* used to successfully treat **PUERPERAL SEPSIS** (**childbirth fever**) in London
* first effective **CHEMOTHERAPEUTIC agent** to cure bacterial infections in humans
PRONTOSIL
76
# **SULFONAMIDES**
what reaction occurs in PRONTOSIL
azo reduction
77
# **SULFONAMIDES**
PRODUCTS of **PRONTOSIL AZO REDUCTION**
Sulfanilamide + Triaminobenzene
78
# **SULFONAMIDES**
* **GERMAN** bacteriologist and pathologist who was awarded the **1939 Nobel Prize** for Physiology or Medicine for his discovery of the antibacterial effects of **PRONTOSIL**
GERHARD DOMAGK
79
# **SULFONAMIDES**
the **FIRST** sulfonamide drugs
PRONTOSIL
80
# **SULFONAMIDES**
* **BRILLIANT AZO RED DYE**
* found to protect against and cure **Streptococcal infections** in **mice**
* it is converted to its active metabolite **"SULFANILAMIDE"**
PRONTOSIL
81
# **SULFONAMIDES**
PRONTOSIL:
**active metabolite**
sulfanilamide
82
# **SULFONAMIDES**
* a generic term that denotes: **ANILINE-substituted** sulfonamides/sulfanilamides
* **prodrugs** that generate active **sulfanilamides**
SULFANILAMIDE
83
# **SULFONAMIDES**
* **NON-aniline** sulfonamide
* used in **BURN patients**
* **NONabsorbable**
MAFENIE
trade name: Sulfamylon
84
# **SULFONAMIDES**
Sulfonamides derived from **p-amino-benzenesulfonamide** are commonly referred to as ____
sulfa drugs
85
# **SULFONAMIDES**
**SULFA drugs** are derived from
p-amino-benzenesulfonamide
86
# **SULFONAMIDES**
era of sulfa drugs
1935
87
# **SULFONAMIDES | STRUCTURE**
the chemical modification of this part of the molecule **INCREASES ACTIVITY** and modifies some **pharmacological properties**
R group
88
# **SULFONAMIDES | SARs**
other **aromatic rings** or introducing other **groups** intro the **benzene ring** will ____ or ____ the **ANTIMICROBIAL activities**
decrease or lose
89
# **SULFONAMIDES | SARs**
____ will **enhance** the **POTENCY**
MONO-substitution
90
# **SULFONAMIDES | SARs**
____ have **BETTER** activities
HETEROCYCLIC rings
91
# **SULFONAMIDES | SARs**
____ will **LOSE** their activities
BIS-substitution
92
# **SULFONAMIDES | SARs**
____ are **essential** for **antimicrobial** activities
UNsubstituted or potential amino group
93
# **SULFONAMIDES | SARs**
**SULFONIC group** must be in the ____ of **ANILINE**
4-position
94
# **SULFONAMIDES | SARs**
____ or ____ **substitution** will **LOSE** the activities
2 or 4-position
95
# **SULFONAMIDES | SARs**
____ wil **DECREASE** the **potency**
other amide group
96
# **SULFONAMIDES | SARs**
* a sulfonamide that is a **structural analog** of **PABA**
* competitively **INHIBITS** the synthesis of **DIHYDROFOLIC ACID** from PABA
SULFAMETHOXAZOLE
97
# **SULFONAMIDES | SARs**
* a **structural analog** of a **portion** of **dihydrofolic acid**
* competitively **INHIBITS** the synthesis of **TETRAHYDROFOLIC acid**
TRIMETHOPRIM
98
# **SULFONAMIDES | SARs**
**PRECURSORS** of **proteins**, **DNA**, **RNA**
Tetrahydrofolic acid
99
# **SULFONAMIDES | SARs**
**STARTING** molecules for the synthesis of **folic acid**
Para-aminobenzoic acid + Pteridine
100
# **SULFONAMIDES | SARs**
**SULFAMETHOXAZOLE** and **DAPSONE** inhibits ____
| **DAPSONE** - tx for **LEPROSY**
dihydro**PTEROATE** synthetase
101
# **SULFONAMIDES | SARs**
**TRIMETHOPRIM** inhibits ____
dihydro**FOLATE** **reductase**
102
# **SULFONAMIDES | SARs**
**Sulfomethoxazole** + **Trimethoprim**
CLOTRIMOXAZOLE
**synergism**
103
# **SULFONAMIDES | ABSORPTION**
achieve **PEAK blood levels** in how many **mins**
30 mins
104
# **SULFONAMIDES | DISTRIBUTION**
highly ____
plasma protein bound
105
# **SULFONAMIDES | DISTRIBUTION**
Sulfonamides given in **LATE TERM** can **INDUCE** ____
neonatal jaundice
106
# **SULFONAMIDES | DISTRIBUTION**
should **NOT** be taken with **LARGE amounts** of **WATER** to prevent ____
CRYSTALLURIA
107
# **SULFONAMIDES | TOXICITY**
**RENAL** toxicity:
**older** sulfonamides
crystalluria
108
# **SULFONAMIDES | TOXICITY**
**BLOOD dyscrasias**
hemolytic anemia
109
# **SULFONAMIDES | TOXICITY**
**DERMAL** toxicity
rashes, pruritus, erythema, SJS
110
# **SULFONAMIDES | TOXICITY**
**RARE** but **serious** SE
hepatitis
drug-induced fever
111
# **SULFONAMIDES | BACTERIAL RESISTANCE**
synthesizing **LARGE** amounts of ____
PABA
112
# **SULFONAMIDES | BACTERIAL RESISTANCE**
____ is **altered** so that it **NO** longer is **inhibitable** by sulfonamides
bacterial dihydropteroate synthetase
113
# **SULFONAMIDES | BACTERIAL RESISTANCE**
bacteria utilize ____ which bypasses **1-carbon synthesis** of **bases**
salvage pathway
114
# **SULFONAMIDES**
spectrum of activity
G+, G-, Nocardia, Chlamydia, Protozoa, Enteric
115
# **SULFONAMIDES**
ADR
CRANK
Crystalluria
Rashes
Anemia
Nausea
Kernicterus
116
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
anti**bacterial**
Sulfa**methizole**
Sulfi**soxazole**
Sulf**acetamide**
Sulfa**chloropyridiazine**
| METH SOX ACET (asset) ni CHLORO
117
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
**PRODRUG** of **Sulfisoxazole**
Sulfisoxazole acetyl
118
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
* salt is prepared by adding **enough DIETHANOLAMINE** to a solution of **SULFISOXAZOLE**
* used in solution for **SYSTEMIC administration**
* used for **installation** of **drops** or **ointments** in the **EYE** for the treatment of **LOCAL EYE INFECTION**
SULFISOXAZOLE DIOLAMINE
119
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
SULFISOXAZOLE DIOLAMINE:
**salt** is **prepared** by **adding enough** ____ to a solution of **sulfisoxazole**
DIETHANOLAMINE
120
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
**MORE SOLUBLE** in **ACIDIC urine**
SULFAMETHAZINE
121
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
SULFAMETHAZINE:
**more solbule** in ____ urine
ACIDIC
122
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
**FIRST agent** for the treatment of **PNEUMONIA**
SULFAPYRIDINE
123
# **SULFONAMIDES | ORAL ABSORBABLE SINGLE**
administered as a **5% solution** in **sterile water IV** for patient requiring an **immediate HIGH BLOOD LEVEL of SULFONAMIDE**
Sulfadiazine sodium
124
# **SULFONAMIDES | ORAL ABSORBABLE MIX**
* available in **oral suspension** and **tablet** form
* contains **equal** amount of **sulfadiazine**, **sulfamerazine**, **sulfamethazine**
TRIsulfapyrimidines
125
# **SULFONAMIDES | ORAL ABSORBABLE MIX**
* tx of ***Plasmodium falciparum*** (px. with **CHLOROQUINE resistance**)
* useful for **PROPHYLAXIS** of **chloroquine resistant** P. falciparum **malaria**
* used for **MALARIA PROPHYLAXIS** for **TRAVELLERS** where **chloroquine resistant malaria** is **ENDEMIC**
Sulfadoxine & Pyrimethamine
126
# **SULFONAMIDES | TOPICAL**
* **VERY soluble** in **water**
* used as **EYE DROPS**
* for **REPEATED topical applications** in the local management of **OPHTHALMIC infections**
Sulfacetamide sodium
127
# **SULFONAMIDES | TOPICAL**
* **SHORT** to **INTERMEDIATE** acting sulfonamide
* **IM**, **IV**
Sulfisoxazole diolamine
128
# **SULFONAMIDES | TOPICAL**
* contains **sulfabenzamide**, **sulfacetamide**, **sulfathiozole**
* as a **VAGINAL cream** in the tx of ***Haemophilus vaginalis***
TRIsulfa
129
# **SULFONAMIDES | TOPICAL**
**TRIsulfa** contains:
sulfa**benzamide**
sulf**acetamide**
sulfa**thiozole**
| nag TRI si BEN ng ACET niya kaya siya ay nakaTHIO
130
# **SULFONAMIDES | ORAL ABSORBABLE MIX**
TRI**sulfapyrimidines** contains **equal** amounts of:
sulfa**diazine**
sulfa**merazine**
sulfa**methazine**
| sina DIA, MERA at METHA ay gumawa ng PYRAMID
131
# **SULFONAMIDES | TOPICAL for BURN**
* homologue of the sulfanilamide molecule that is **NOT inhibited** by **PABA**
* effective against ***Clostridium welchii*** and for the **prophylaxis** for **wounds**
Mafenide acetate
132
# **SULFONAMIDES | TOPICAL for BURN**
* tx of infection against ***Pseudomonas spp.***
* a **VERY POTENT** antimicrobial in the treatment of **burns**, **scald**, and **wound infections**
* **PATIENT ACCEPTANCE** is **BETTER** than **mafenide**
Silver sulfadiazine and zinc salt
133
# **SULFONAMIDES | TOPICAL for BURN**
why is the **PATIENT ACCEPTANCE** of **Silver sulfadiazine and zinc salt** BETTER than MAFENIDE?
bc it does not cause systemic acidosis
134
# **SULFONILAMIDES | INTESTINAL, ULCERATIVE, BACTERIAL FLORA**
* effectivev in treating **ULCERATIVE COLITIS**
Sulfasalazine
135
# **SULFONILAMIDES | INTESTINAL, ULCERATIVE, BACTERIAL FLORA**
SULFASALAZINE:
**prodrug**
5-aminosalicylic acid & sulfapyridine
136
needed for **BACTERIAL GROWTH** and **CELL DIVISION**
Dihydrofolate Reductase inhibitors
137
# **DIHYDROFOLATE REDUCTASE INHIBITORS**
* closely related to several anti-**malarials**
* a **potent** anti**bacterial**
* tx of **UNCOMPLICATED UTI**
Trimethoprim
138
# **DIHYDROFOLATE REDUCTASE INHIBITORS**
* tx of **CHRONIC UTI**
* DOC for booth **COMPLICATED** and **UNCOMPLICATED UTI** especially caused by **ENTEROBACTERIA**
Sulfamethoxazole & Trimethoprim
139
# **UNTOWARD EFFECTS OF SULFONAMIDES**
**HEMATOPOIETIC** system
hemolytic anemia
(in **G6PD deficient** patients)
140
# **UNTOWARD EFFECTS OF SULFONAMIDES**
**URINARY** tract
occlusions due to precipitates
141
# **UNTOWARD EFFECTS OF SULFONAMIDES**
DRUG INTERACTION
high affinity to plasma proteins
142
**Sulfonamides** are used only when a **particular agent is known to be** ____ or ____ than other antibiotics for particular infeciton
equal or better
143
when **sulfonamide** is used **SYSTEMICALLY**:
____ and ____ must be **monitored closely**
hematopoietic system & renal function
144
when **sulfonamide** is used **SYSTEMICALLY**:
the patient must be given **sufficient amount of water** to produce ____ of **urine**
1.2 L / day
145
* reported to be effective against **MALARIA** and **RICKETTSIAL** infections
* MOA: **same** with **sulfonamides**
* **CROSS RESISTANCE** to sulfonamides
* mainly used for treating **LEPROSY** caused by ***M. leprae***
SULFONES
146
# **SULFONES**
reported to be effeective against ____ and ____ infections
malaria and rickettsial
147
# **SULFONES**
MOA
same w sulfonamides
148
# **SULFONES**
CROSS RESISTANCE to ____
sulfonamides
149
LEPROSY is also known as
Hansen's disease
150
# **SULFONES**
aside from **rodents (mice)** ____ is another **biological test animal** to culture M. leprae
ARMADILLO
151
# **SULFONES | DAPSONE STRUCTURE**
**susbtitution** on both ____ and ____ functional groups
4- and 4'-amino
152
# **SULFONES | DAPSONE STRUCTURE**
____ on ONLY **ONE AMINO** functional group
MONOsubstitution
153
# **SULFONES | DAPSONE STRUCTURE**
____ on the **BENZENOID RINGS**
Nuclear substitution
154
# **SULFONES | DAPSONE STRUCTURE**
**replacement** of **ONE** of the **PHENYL ring** with a ____
heterocyclic ring
155
# **SULFONES**
DAPSONE:
**parent compound**
sulfone
156
# **SULFONES**
**PROTOTYPE** of sulfone
DAPSONE
157
# **SULFONES**
* treatment of both **LEPROMATOUS** and **TUBERCULOID** leprosy
* DOC: **DERMATITIS HERPETIFORMIS**
* sometimes used with **pyrimethamine** for the tx of **MALARIA** and with **TMP** for **PCP**
* SE: hemolytic anemia, methemoglobinemia, toxic hepatic effects
DAPSONE
158
# **SULFONES**
DAPSONE:
**DOC**
dermatitis herpetiformis
159
# **SULFONES**
DAPSONE:
sometimes used with ____ for the tx of **MALARIA**
pyrimethamine
160
# **SULFONES**
DAPSONE:
sometimes used with ____ for **PCP**
Trimethoprim
