ANXIOLYTICS & HYPNOTIC DRUGS Classification: 1. Benzodiazepines 2. Barbiturates 3. Non benzodiazepine and non barbiturates 4. Buspirone 5.

adrenoceptor antagonist 6. Diphenhydramine is an antihistamine used as sleeping pills particularly in wakeful children 1. Benzodiazepines: i) Midazolam: is ultra short acting , used as I.V. anaesthetic Ii)Alprazolam: has anxiolytic & anti depressant property iii)Diazepam: Used I.V for the treatment of status epilepticus iv) Clonazepam: is an anxiolytic drug especially in mania v)Flumazenil: Benzodiazepam antagonist vi) 1-selective Benzodiazepam: will be having anxiolytic property but no sedation vii) 2- selective Benzodiazepam: anxiolytic and muscle relaxant property

Benzodiazepam doesnot effect random eye movement sleep(REM) Benzodiazepam doesnot effect growth hormone secretions Mostly they undergo metabolism by glucoronidation Hydroxy diazepam is called as Timazepam Hydroxy nor diazepam is called as Oxazepam Ioverdoses Benzodiazepam prolongs sllep without serious depression of respiratory (or) cardiovascular functions Short acting benzodiazepams cause severe withdrawal symptoms Severe psychological & physiological dependence occurs with Benzodiazepams Fumazenil can be used to reverse the effects of Benzodiazepines over doses Half life of Fumazenil 2hrs Fumazenil when given with Tricyclic anti depressants(TCA) precipates convulsions Is a partial 5HT-1a agonist Ipsapirane & Jepirone are analogues to Buspirone 5HT receptors are anti inhibitory in nature Buspirone also shows activity of non- adrenergic in local cerulus region It takes several days to weeks to show action It is ineffective in controlling franic attacks (or)severe anxiety states It does not produce sedation or motor in- coordination

Pharmacokinetics:

2.Buspirone:

3.Barbiturates:

They are potent cyp enzyme inducers Phenobarbitol is used for treatment of epilepsy Thiopental ultra short acting Given I.V. for anaesthetic action Barbiturates are dangerous to patients suffering from metabolic diseases like porphyration condition

Serotonin selective reuptake inhibitors(SSRI) such as fluoxatin, peroxitin, sulfranil can also be used for anxiety disorders

Anti-epileptic drugs: like -pentin , vigabatrin, Tiagabine , valproate can also be used as anxiolytic 5HT3- receptor antagonists: Ondansetron can also show anxiolytic activity ANALGESICS Morphine:

Supra spinal analgesia of morphine is because of -receptor antagonistic property For final analgesic action & receptors Respiratory depression, pupil constriction, euphoria & physical dependence is due to -receptors Disphoria is due to receptors Respiratory depression by opiates is not accompanied by depression of medullary centres controlling cardiovascular function Respiratory depression is most common cause of opiate poisoning Pin point pupil is characteristic of opiate poisoning Morphine inhibits peristaltic movements resulting in constipation Opiates should be avoided in biliary colic pains due to gall stones It increases concentration of amylase & lipases in plasma Morphine releases histamines from mast cells & causes itching at the site of injection Promotes bronchoconstriction & hypotension where as pethidine doesnot produce these effects is a phenomena of raising & stiffening of tail of rat & mice given opiate drugs It is the technique for screeing morphine like drugs Opiates suppresses immune system which produces tolerance and dependence Clonidine & ketamine are used to Alliviate avstinence syndrome Half life of morphine 3-6hrs Morphine 6-glucuronate is more active analgesic than morphine Morphine 3-glucuronate acts as antagonist for analgesic effect of morphine Morphine glucuronates undergoes extrinsic hepatic cycle Morphine like drugs have longer duration of action in Neonates because of low conjugation reaction hence contraindicated during child birth

Strace state:

Pharmacokinetics:

Unwanted effects: Coma, respiratory depression with characteristic constricted pupil Diamorphine:

Di-acetylated derivative of morphine also called as Heroin Can cross BBB more rapidly than morphine 3 methyl morphine or 3 methoxy morphine Oral analgesic for mild pains Doesnot produce Euphoria Used in combination with paracetamol for analgesic action Most common side effect Constipation Mostly used as anti-tussive agents in cough syrups

Codeine:

Pethidine: 2

Also called as mepridine It produces restlessness Metabolism is mainly due to N-methylation Pethidine is preferred to morphine during labour because it doesnot reduce force of uterine contraction Excitement, hyperthermia, convulsions when given along with MAO inhibitors Metabolite of pethidine is norpethidine is responsible for these side effects Highly potent Used in severe chronic pains 1000 times more potent than morphine Used for veterinary purposes Is a longer acting opiod analgesic Half life 24hrs Less sedation Widely used for treating morphine & diamorphine addiction It is a mixed agonist & antagonist with analgesic action similar to morphine Produces dysphoria, nightmares & hallucinations Hallucinations occur because pentazocin acts on -receptor which is not opiod receptor Pure partial receptor agonist It doesnot have any side effects like euphoria, dysphoria, respiratory depression It is a shorter acting drug produces sedation & atropine like side effects Weak agonist at receptors Weak inhibitor of nor adrenergic reuptake opiod antagonists:

Side effects:

Pentanide & Isopentanyl phosphate:

Atropine

Methadone:

Pentazocin:

Duprenorphine:

Mepazinol:

Tremadol:

Nalorphine:

Higher doses mimic the actions of morphine Can produce physical dependence & also withdrawal syndromes First pure opiod antagonist with affinity for all 3 opiod receptors Also shows ocupuncture analgesia which is associated with opiod release Fo treatment of respiratory depression caused by opiates during labour Halflife 2-4hrs should be given repeatedly Precipitation and withdrawal syndromes

Naloxone:

Clinical use:

Side effect

Naltrexone: Similar to naloxane but longer acting Paracetamol: 3

Analgesic & anti-pyretic effect by lacking anti-inflammatory effects Selective to COX 3 enzyme Half life 3hrs Overdoses produce severe hepatotoxicity

Tricyclic antidepressants(TCA): Amipramine & Amytryptaline: for treatment of neuropathic pains Antiepileptic drugs:

-pentin, phenytoin, carbamazepine are used for neuropathic pain ketamine an analgesic drug shows wind up phenomemon I.V. lignocaine is effective in neuropathic pain

Enkephalins: Ex: Thiorphan Metabolic degradation of opiate peptides & acts as analgesic drugs Epibatidine:

Nicotinic Ach receptor agonist Also a potent analgesic drug Agonist at cannabinoid receptor Also acts as an analgesic drug ANTIDEPRESSANTS

Tetrahydro cannabinol:

Classification: i)Mono Amine Uptake Inhibitors: a)Non selective: TCAs (e.g.imipramine,amitriptyline) b)Other Non selective: TCAs: Venlafaxine, Duloxetin, Buproprion, St.Johns wort Nortryptaline & Desipramie: Selective for noradrenaline reuptake Clomipramine: Used for antidepressant and antianxiety Venlafaxine:

Used for treatment resistant patients Rapid action than other antidepressants Safer in higher doses Hyperforin should not be taken with cyclosporin or other antidiabetic dugs because their activity decreases Cyp enzyme inducer weak inhibitor of dopamine & NA uptake mechanism mainly used in depression associated with anxiety slow release formulations are used to treat nicotine dependence hydroxyl desmethyl imipramine selectively inhibits NA uptake & has no effect on 5HT TCAs produces sedation except Buproprion which produces insomnia In higher doses TCA prolongs QT interval

St.johns wort(Hypericum):

Buproprion:

Imp points:

TCA potentiates action of alcohol as anaesthetic agents & causes severe respiratory depression For moderate to severe endogenous depression especially with psychomotor features like insomnia Sedating antidepressant drug amitryptiline is used For short term treatment of nocturnal aneuresis in older children Imipramine is used

Selective Serotonin Reuptake Inhibitors(SSRI): Fluoxetine, fluvoxamine, paroxetine, sertaline, citalopram-these are used for treatment of anxiety disorder known as obsessive compulsive disorder Fluoxetine:

long acting SSRI half life 48hrs

Peroxitin & fluoxotin: should not be used in combination with TCA because they are cyp enzyme inhibitor Unwanted effects:

Insomnia, loss of libido and failure of orgasm In combination with MAO Is, SSRIs can cause serotonin syndrome characterized by tremors, hyperthermia, & cardiovascular collapse Selective serotonin reuptake inhibitor Active in E form

Citalopram:

MAOI: EX:Phenelzine, tranylcypramine, and iproniazid

Irreversibly inhibits MAO enzyme Selegaline is specific selective MAO B inhibitor Meclobimide, clorgiline MAO A selective MAOI areused in the treatment of parkinsonism NA & 5HT are selective substrates for MAO enzyme Phenylethylamine & benzylamine are specific substrates for MAO B Dopamine & Tyramine are non selective Non selective MAOI promote cheese reaction Moclobimide, selegaline, clorgiline do not provoke cheese reaction MAOI should not be given with pethidine TCAs should not be taken with MAOI

Miscellaneous antidepressants: Trazadone: is a weak 5HT uptake inhibitor, also inhibits 5HT & H1 receptors Nefarodone & Mianserin:

similar to that of Trazadone safer in high doses inhibitory action on 2 receptors,5HT2 & 5HT3 receptors faster onset of action compared to other drugs

Mirtazapine:

Mood stabilizing drugs: Lithium, carbamazepine, valproate, -pentin Lithium:

It can be used as an adjuvant to antidepressant drugs in severe cases of unipolar depression

Inosital mono phosphate is an inhibitor and blocks IP3 pathway Narrow therapeutic index drug Inhibits glycogen synthase kinase & inhibits apoptosis & amylide formation Polyuria( inhibits ADH), thyroid hypothyroidism, weight gain enlargement ,sometimes associated with

Side effects:

Acute lithium toxicity results in neurological effects leads to death of the person if plasma concentration reaches 3-5 m mol/lit GENERAL ANAESTHETICS

Inhalation anaesthetics: Propofol, ether, dichloroethylene, cyclopropane, methoxyflurane, nflurane, isoflurane, sevoflurane, desflurane , nitric oxide Ether:

Produces respiratory irritation Induction time is very slow Explosive in nature Widely uised inhalational anaesthetic Produces malignant hyperthermia Metabolic product is trifluoro acetate

Halothane:

Side effect: cardiac arrhythmia & hepatotoxicity Nitroprusside:

Results in bone marrow depression Increases risk of anaemia related to vitB12 deficiency Increases frequency of abortion & abnormal foetal abnormalities side effect of enflurane is convulsions(seizures) produces malignant hyperthermia most widely used volatile anaesthetic causes hypotension due to coronary activity exacerbate cardiac ischaemia in patients with coronary disease because of steal phenomena used for day case surgery mainly causes respiratory tract irritation which leads to cough & bronchospasm No respiratory irritation but produces malignant hyperthermia Side effect: renal toxicity

Enflurane:

Isoflurane:

Desflurane:

sevoflurane:

I.V. anasthetics: Thiopental:

Ultra short acting barbiturate can cause unconsciousness with in 20sec and lasts about for 5-10 min Slowly metabolized because of high lipophilic character Side effect:cardio vascular depression It has no analgesic property

If injected into local tissues produce necrosis & ulceration,immediate injection of procaine through same needle is recommended if this accident occurs Contraindicated in porphyria patients Hang over effects are seen with thiopental Larger therapeutic index compared to thiopental On prolonged therapy suppresses the production of adrenal steroids It should not be used in patients with adrenal insufficiency Induces involuntary movements during induction Metabolized very rapidly hence given as continuous infusion Particularly used in day case surgery analogue of phencyclidine( called as steet drug) NMDA receptor antagonist It takes 2-5 min for inducing anesthesia Produces dissociative anesthetic action Produces cardiovascular or respiratory depression Increases intracranial pressure Produces cerebral ischaemia The main drawback of ketamine is hallucinations delution & irritational behavior

Etomidate:

Propofol:

Ketamine:

Unwanted effects:

Drug interaction: Ketamine+benzodiazepam- used to induce anaesthetic activity in children Midazolam:

Ultra short acting benzodiazepam Doesnot cause respiratory or cardiac depression It is often used as pre operative sedative & during endoscopy where complete anaesthesia is not required GASTRO INTESTINAL TRACT

Classification: i)Drugs used to inhibit or neutralize gastric acid secretion: a)Antacids: Magnesium hydroxide:

Insoluble powder that produces Mgcl in stomach Doesnot produce systemic alkalosis Prolonged anti acid effect Inhibits absorption of pepsin Side effect: Diarrhoea Forms Aluminium chloride(Alcl3) in stomach Increases gastric pH to 4 Inhibits absorption of pepsin

Magnesium trisilicate:

Aluminium hydroxide gel:

Colloidal AlOH combines with phosphate & increases the excretion of phosphate in feaces that results in decreased excretion of phosphate via kidneys (in treating patients with chronic renal failure) Increases gastric pH to 7.4 Releases CO2 & inturn stimulates gastric secretions(releasing of CO2 is called as Bulching effect) Side effect:Systemic alkalosis

NaHCO3:

Alginates are combined with antacids for relieving bloating & flatulence H2 receptor antagonists:

Cimetidine inhibits cyp enzymes but its adverse effect is that it produces gynacomastia & inhibits sexual functions Ex:ranitidine, nizatidine,famotidine Cimetidine potentiates actions of oral anticoagulants & TCA In general H2 antagonists produce alopecia & hyper gastrinaemia Derivatives of Benzimidazole They irreversibly inhibit H+/k pump irreversibly Ex:Esmaprazole,lansoprazole,pantoprazole,rabiprazole These are weak bases They degrade rapidly at low pH hence taken as enteric coated granules Half life is 1hr but effect acid secretions for 2-3 days Unwanted effect:

Proton pump inhibitors(PPI):

Phaermacokinetics:

Diarrhoea, impotency, gynacomastia Note: should be used cautiously in patients with liver diseases Treatment of H.pylori: Triple therapy which comprises of PPI, in combination with amoxicillin & metranidazole or clarithromycin b)Drugs that protect mucosa: Ex:Bismuth chelates:

Used in combination to treat H.pylori Inhibits bacterial proteolytic enzymes In renal failure condition Bismuth chelates triggers encephalopathy

Unwanted effects: Blackening of tongue and feaces Sucralfate:

Complex of AlOH & sulfated sucrose Given orally in the acid environment forms polymers & present in stomach for 3hrs after administration

Drug interaction: Fluoroquinolones , thiophylline, tetracyclines, digoxin, & amytryptyline should not be given with sucralfate Unwanted effect: constipation Note: It should be used with consciousness in pregnancy & lactational women iii) Misoprostal:

Stable analogue of PGE

Prevents gastric damage with chronic use of NSAIDS Exerts direct action on parietal cells inhibiting the basal secretions of gastric acid

Unwanted effects: Diarrhoea, uterine contraction (should not be used in pregnancy) ANTIEMETIC DRUGS i)H1 receptor antagonists:

Ex:cinnargine, meclizine, cyclizine, promethazine Promethazine is used inmorning sickness of pregnancy & has been used for space motion sickness Cinnarzine & cyclizine-for motion sickness Cinnarzine is also used for menieres disease Ex:Hyoscine or scopolamine For motion sickness given by transdermal patch Ondansetron, granisetron, tropicetron,dolcetron Mainly used for cisplatin induced emesis Ex;Tolpromazine, perfenazine, prochlorperazine, trifluperzine These are effective in treating severe forms of emesis

ii)Muscarinic antagonists:

iii)5HT3 receptor antagonists:

iv)Dopamine antagonists:

Unwanted effects: Extra pyramidal effects , hypotension, sedation Metachlorpromide:

D2 antagonist Realated to phenothiazine family acts aon CTZ & produce antiemetic action Crosses BBB

Unwanted effects: Extra pyramidal effects(EPE), increased prolactin levels resulting in galactorrhoea , occulogyric crises Domperidon: Similar to metachlopromide but does not cross BBB(No EPE) Cannabinoids:

Nabilone inhibits vomiting when taken by oral route It effectively antagonizes CTZ stimulated emesis

Unwanted effects: drowsiness, postural hypotension, hallucinations Steroids & neurokinin antagonists:

Dexamethasone can be used alone but often used with phenithiazine It is used in high doses I antagonist:Ex: Eprepipant

Neurokinin

DRUGS THAT INCREASE MOTILITY OF GIT i)Bulk & osmotic laxatives

Ex:methyl cellulose, sterculia, agar, bran, ispaghula husk They take several days to show their action For slow purgation ispaghula is drug of choice All are polysaccharides Ex: lactulose semi synthetic disaccharide of fructose & galactose

ii)Osmotic laxatives:

It takes 2-3 days to act

Unwanted effects: Induces peristalisis ,doarrhoea and flatulence Faecal softeners: i)Docusate sodium: detergent like action produces soft feaces ii)Arachis oil & liquid paraffin: it also acts as feacal softener stimulant laxatives:

Ex:Bisacodyl , Sodium picosulfate Bisacodyl stimulates rectal mucosa & induces defecation in 15-30 min Sodium picosulfate & Docusate sodium have similar properties Sodium picosulfate is given orally in preparing for intestinal surgery or colonoscopy

iv)senna & anthraquinone glycosides: Directly stimulates myenteric plexus , increases peristalisis & thus cause defeacation Unwanted effect: skin irritation & Carcinogenicity Prokinetic agents: Ex:Domperidone, metaclopromide & cisapride Cisapride:5HT4 agonist prolongs QT interval resulting in arrhythmia ANTIDIARRHOEAL AGENTS There are 3 approaches to treat severe acutediarrhoea i)Maintainence of fluids & electrolyte balance ii)Use of anti-infective agents iii)Use of spasmolytics & other anti-diarrhoeal agents Most common bacteria encountered is E.coli and it requires the antibiotics like erythromycin & ciprofloxacin for treatment ANTIMOTILITY & SPASMOLYTICS Atropine+Diphenhydramine are used in combination Morphine derivatives: Morphine congeners like codeine, pethidine Loperamide:

It is the drug of choice for travelers diarrhea Doesnot cross BBB but shows similar actions like morphine Abdobinal cramps Should not be used for children

Side effect:

Diphenoxylates: They are taken along with atropine Drugs that inhibit spasm in the gut are also used in irritable bowel syndrome Ex:Propantheline,Dicyclovirine,Mebivarine Absorbents:

Ex:Kaolin, pectin, methyl cellulose, activated attapulgite(Mg. Al.Silicate) Kaolin+morphine mixture is official in B.P.

Drugs for chronic bowel diseases Ex:Glucocorticoids: These are used because of its potent anti-inflammatory activity Drug of choice:Budisonide,Prednisalone Aminosalicylates: Sufasalazine: is a combination of 10

sulfapyridine + 5-amino salycilic acid MOA: Inhibits inflammation by scavengering free radicals, inhibits PG & leucotriene production & by inhibits chemotaxis & sucroxide generation Mesalazine:5-amino salycilic acid Oxalazine: 2 molecules of 5-amino salycilic acid linked with diazobond which can be broken by colonic bacteria Valsalazine: 2 molecules Balsalazine:4amino salicylic acid Other drugs:Azithioprine, 6-mercapto purine cytokine inhibitor infliximab or Sodium chromoglycate DRUGS AFFECTING BILIARY SYSTEM

Ex:cholesterol, cholilithiasis Principle agent is urso deoxycholic acid Atropine is commonly used to relieve biliary spasm used in combination with morphine Organonitrates can also be used Morphine alone cannot be used

DRUGS AFFECTING BILIARY SPASMS

CHEMOTHERAPY ANTI-VIRAL DRUGS ANTI HIV DRUGS I)Nucleoside reverse transcriptase inhibitors: Ex: Zidovudine

Is an analogue of Thymidine It is used in individuals who are associated with dementia given to parturient mother We can reduce mother to baby transmission(if nevirapine is there in options nevirapin should be prefered)

Didanosine: is an analogue of deoxy adenosine Zalcitabine:

is an homologue of cytosine It is activated in T-cells by a different phosphorylation pathway from Zidovudine

Lamuvudine: is an analogue of cytosine. It is also used in the treatment of hepatitis B Stavudine: It is an analogue of Thymidine Abacavir: It is a guanosine analogue ii)Non-nucleoside reverse transcriptase inhibitors: MOA:They bind to the reverse transcriptase enzyme near the catalytic site and denature it. Nevirapine: It can prevent mother to baby transmission of HIV if given to parturient mother & the neonate Efavirenz: 99% protein bound drug and has the longest half life in nucleoside reverse transcriptase inhibiting activity around 50hrs. Mefloquine: is the longest acting drug for 30 days iii)Protease inhibitors: 1.Saquinavir 2.Nelfinavir 3.Indinavir 4.Ritonavir 11

5.Amprenavir -Highest CSF concentrations can be seen with Indinavir -Lowest CSF concentrations can be seen with Saquinavir Unwanted effects:

Diabetes(hyper glycaemic condition) Rhabdomyolysis Nevirapine & Ritonavir should be taken along with food Saquinavir should be taken within 2hrs of meal

iii)DNA polymerase inhibitors: Ex:Aciclovir:

It is a guanosine derivative It is used in the treatment of Herpes simplex It is also used for the treatment of Voricella zoster infections & Epstein-Barr virus infections Aciclovir is converted to monophosphate by thymidine kinase Thymidine kinase is virus specific form of enzyme The host cell kinases then convert the monophosphate to trisphosphate It is the acyclovir trisphosphate that inhibits viral DNA polymerase terminating thenucleotide chain Aciclovir acts as chain terminator It can be given Orally, I.V. , & topically Contraindicated in renal dysfunction Local inflammation with I.V. injection

MOA:

Unwanted effects:

Valaciclovir is the prodrug of Aciclovir Famciclovir undergoes metabolism resulting in the formation of active metabolite compound called Penciclovir Ganciclovir:
o o o o o

It is an acyclic analogue of guanosine It is the drug of choice for cytomegalovirus promotes bladder cancer Mechanism of action is similar to acyclovir but unlike acyclovir it doesnot act as a chain terminator It is given by I.V. route It produces severe bone marrow depression It is a synthetic nucleoside , similar to structure to guanosine It acts by altering virus nucleoside pool or by interfering with the synthesis of mRNA. In aerosol form it is used in the treatment of influenza and infections with respiratory syncytial virus It is also used in the treatment of hepatitis C as well as lassa fever caused because of arenavirus infections It is a synthetic non nucleoside analogue of pyrophosphate that inhibits the viral DNA polymerase by bindibg directly to the pyrophosphate-binding site

Tribavarin(ribavarin):
o o o o

Foscarnet(Phosphonoformate):
o

12

o o

It is a second line of drug in cytomegalo virus infections It causes severe nephrotoxicity

iv) Inhibitors of HIv fusion with host cells: Ex: Enfurvirtide: It is given by sub cutaneous route v)Neuraminidase inhibitors and inhibitors of viral coat assembly:
o o o o

Zanamivir and Oseltamivir are used in treating swine-flu infections These are active against both influenza A & influenza B virus Zanamivir is available as a powder for inhalation Oseltamivir is available as an oral preparation It blocks M2 ion channels , thus inhibiting viral disassembly It is active against influenza A but not influenza B It is also used in the treatment of parkinsonism

Amantadine:
o o o

Vi) Biologics and immunomodulators: Immunoglobulin Palivisumab:

o o

It is a monoclonal antibody used in respiratory and viral infection It is given by I.M. route

Interferons(,,): Interferon : produced by T-lymphocytes they are called as immune interferon Interferon (,): produced by B and T lymphocytes,macrophages and fibroblasts MOA:
o o

Binds to specific ganglionic receptors on host cell membrane and also inhibits translaton of viral mRNA into viral proteins They donot cross BBB Interferon 2a is used for the treatment of h$epatitis B infections and AIDSrelated Kaposi sarcomas. Interferon 2b is used in the treatment of hepatitis C Preparations of IFNs conjugated with polyethylene glycol(pegylated IFNs) have a longer lifetime

Clinical uses:
o o o

Unwanted effects: Alopecia,bone marrow depression,cardio vascular & thyroid problems Ionosine pranobex: Immunomodulator interferes with viral nucleic acid synthesis & also promotes immune potentiation HAART therapy: -Highly active anti-retro viral therapy -In this 2 nucleoside reverse transcriptase inhibitors+a non nucleoside transcriptase inhibitor(or) 2 protease inhibitors ANTI-FUNGAL DRUGS Amphotericin: Source: cultures of streptomyces
o o o o

It is a polyene antibiotic It mainly interferes with permeability & transport functions of cell membrane They cause loss of intracellular potassium It is a good standard for treating Aspergillus & candida infections

Drug interaction: 13

Amphotericin+flucytosine= synergistic action Pharmacokinetics:

It can be given orally, topically or by I.V route For I.V. route it is complexed with liposomes or lipid containing preparations Amphotericin+flucytosine is used in the treatment of cryptococcal meningitis Serious side effect is renal toxicity Common side effects are hypokalaemia, hypomagnesinaemia,anaemia,anaphylactic reaction If given by I.V. produces flebitis(inflammation) If given by intrathecal infusion produces neurotoxicity No absorption on mucous membrane Used for GIT infections It is a narrow spectrum antifungal agent Source:pencillium griseofulvum It is a fungistatic Interacts with fungal microtubules & interferes with mitosis Potentially induces cytochrome p450 enzyme Photosensitivity reactions Contraindicated in pregnanat woman It comprises of a ring of 6 amino acids Based on the structures of echinocandin B

Unwanted effects:

Nystatin(fungicidin):

Griseofulvin:

MOA:

Unwanted effects:

Echinocandins:

MOA: They inhibit the synthesis of 1,3 glucan a glucose polymer necessary for the maintainence of fungal cell wall Caspofungin:

It can be used for treatment of invasive aspergillosis that are refractory to amphotericin It is given by I.V. once daily

Synthetic antifungal agents: i)Azoles: MOA:

Inhibits fungal cyt p 450,3a enzyme i.e., lanosine 14--demethylase which converts lanosterol to ergosterol Azoles also inhibits transformation of candidal yeast cells to hyphae

Drug interaction: Azoles+Amphotericin= decreases the action of Amphotericin 1.Ketaconazole:used for systemic fungal infection Unwanted effects: Liver toxicity(valproate also shows liver toxicity)

14

-It also inhibits adrenocorticosteroids& testosterone synthesis when given in higher concentrations Ciclosporin,terbinafine,astemizole increase plasma concentrations of ketaconazole Rifampicin:H2 receptor antagonist and antacids Decreases absorption of ketaconazole Flucanazole: Drug of choice for fungal meningitis Shows fungicidal action Unwanted effects: Stevens johnsons syndrome(skin infections) Itraconazole:

Active against dermatophytes Undergoes extensive hepatic first pass metabolism Doesnot penetrate CSF

Unwanted effects: Stevens johnsons syndrome(skin infections) Inhibits cyp enzyme similar to that of ketaconazole Miconazole: given for fungal infections in bone joints& lung tissues Side effects:Blood dyscariasis(poisoning),Hyponatraemia Clotrimazole,econazole,tioconazole, Sulconazole are used only for topical applications -Clotrimazole interferes with the aminoacid transport into the fungus Flucytosine: given along with amphotericin for cryptococcal meningitis MOA:Flucytosine is converted to the antimetabolite 5-fluorouracil in fungalbut not human cells.5-fluorouracil inhibits thymidylate synthase and thus DNA synthesis Unwanted effects:causes nephrotoxicity Anti cancer side effects Terbinafin:

Highly lipophilic,keratinophilic,fungicidal compound It is mainly used for nail infections

MOA:inhibits squalene epoxidase enzyme Naftifine : similar to terbinafin Amorolfine:It is a morpholine analogue ( blocker containing morpholine ring is timolol) ANTIHELMINTHICS 1.Benzimidazoles: i)mebendazole ii)thiabendazole iii)Albendazole MOA:Inhibits polymerization helminth tubulin thus inhibits microtubule dependent functions such as glucose uptake -Fatty meals increase the absorption of mebendazole Unwanted effects: Gastro intestinal disturbances (common for all antihelminthics) Albendazole: 15

Undergoes metabolism & results in the formation of sulfoxide & sulfone metabolites Mebendazole is contraindicated in pregnancy & children below the age of two Broad spectrum antihelminthic drug Drug of choice for all forms of schistosomiasis

Praziquantel:

MOA: Disturbs Ca+ homeostasis by binding toprotein kinase C-binding sites in -sub unit of voltage gated Ca+ channels MOA2:

Praziquantel also disturbs the tegument of the parasite unmasking novel antigen & increases susceptibility to the host normal immune responses It is also effective in cysticercosis It is considered to be a safe drug with minimal side effect

It is the drug of choice for tape worm infection It can be given to pregnant & lactating woman Side effect: Low grade fever Piperazine:

Used for the treatment of round & thread worms It reversibly inhibits neuromuscular transmission(NMT) by activating GABA-gated clchannels Polarized worms are expelled alive in condition

Unwanted effects: Bronchospasms , It should not be given to pregnant patients or to those with renal or hepatic dysfunction Niclosamide: Widely used for the treatment of tape worm infections MOA:

Scolex and the proximal segments are irreversibly damaged For taenia solium infections the drug is given in single dose after a light meal followed by a purgative 2hrs later

Side effect: promote cysticercosis Diethyl carbamazine citrate(DEC):

DEC is a piperazine derivative Drug of choice for Bancrofti infections & lovalova infections It interfers with helminthic arachidonate acid metabolism It makes the parasite susceptible for host immune responses Enlargement of lymph glands Tachycardia Respiratory disturbances It should not be used in the treatment of onchocerciasis An antihelminthic drug showing immunostimulant activity Increases IL2 expression It shows nicotinic like action(stimulating & subsequent blocking of neuromuscular junction[NMJ])

MOA:

Unwanted effects:

Levamisole:

Side effects: Encephalopathy 16

It can cross BBB Ivermectin:

o o o

Broad spectrum antiparasitic drug Drug of choice for filarial infections and also effective in the treatment of onchocerciasis which causes onchocercal blindness Can be used in the treatment of elephantiasis

MOA: It opens glutamate gated cl-channels which are present only in invertebrates Unwanted effects:
o

Enlargement of lymph glands

Verapamil can partially reverse Benzimidazole resistance in trypanosomes ANTICANCER DRUGS i)Nitrogen mustards Cyclophosphamide:
o o o o o

Active form-phospharamide mustard Toxic metabolite: Acrolein It has an effect immunosuppressant on lymphocytes and hence can be used as

Antidote for acrolein is MESNA or N-acetyl cysteine (MESNA-Sodium-2-mercapto ethane sulfone)

Estramustine: Chlormethine(mustine)+estrogen= used for the treatment of prostate cancer ii)Nitroso ureas: lomustine and carmustine are highly lipophilic hence used for treatment of brain tumours Busulfan:

Selectively suppresses bone marrow depressing the formation of granulocytes & platelets Used in the treatment of chronic granulocytic leukamaeia(Blood cancer)

iii)Platinum compounds: Cisplatin:

it causes intra strand cross linking between N7 & O6 of adjacent guanosine molecules resulting in local denaturation mainly used in the treatment of solid tumours along with taxol I.V. injection produces severe nephrotoxicity(foscarnet,amphotericin,&cisplatin also show nephrotoxicity) In order to overcome nephrotoxicity of cisplatin more amount of water should be taken

Side effect: Vomiting can be treated with 5HT antagonists(ondansetron,gramisetron) Carboplatin: produces less nephrotoxicity but more myelotoxic Dacarbazine: prodrug activated in liver ,resulting compound is subsequently cleaved in the target cell to release an alkylating derivative Temozolimide: Used for the treatment of malignant glioma iv)Antimetabolites: Methotrexate:

It contains pteridine ring(PABA & glutamic acid) They donot cross BBB

Unwanted effects: 17

Folic acid deficiency it can be treated with folinic acid(active form of folic acid is poly glutamate form) v)pyrimidine analogues: Fluorouracil:

Inhibits thymidilate synthase enzyme Given by parenteral route causes myelotoxicity & cerebral disturbances Raltitrexed inhibits thymidilate synthase enzyme Pemetrxed inhibits thymidilate transferase

Capecitabine: undergoes metabolism to form fluorouracil Cytarabine(cytosine arabinoside):

is an analogue of nucleoside 2-deoxycytidine Inhibits DNA polymerase enzyme

Gemcitabine: analogue of citarabine Given in combination with cisplatin Side effect: Influenza like syndrome vi)Purine analogues: 1.Pentostatin 2.mercaptopurine 3.thioguanine 4.fludarabine Pentostatin inhibits adenosine deaminase enzyme important to convert adenosine to inosine. vi)cytotoxic antibiotics: They mainly contain anthracyclines 1.doxorubicin 2.Idarubicin 3.Epirubicin 4.Mitoxantrone Side effect: cardiotoxicity Inhibits DNA gyrase (or) Topoisomerase Dactinomycin:

Doesnot produce cardiotoxicity Mainly used for paediatric cancer Metal chelating glycopeptides antibiotic Degrades DNA causes chain fragmentation Most effective in G2 phase of cell cycle, mitosis & also G0 phase

Bleomycin:

Side effect: pulmonary fibrosis, hyperpyrexia Mitomycin:

Preferentially acts on O6 of guanosine nucleus Produces nephro & pulmonary toxicity Inhibits DNA & RNA synthesis and interferes with mitosis at interphase Used for the treatment of Hodgkins disease It causes disulfiram like actions

Procarbazine:

18

As it is a weak MAO inhibitor it produces hypertension when it is given with sympathomimetic agents Produces blood cancer It is an urea analogue Inhibits ribonucleotide reductase Enzyme Mainly used for the treatment of blood cancer

Hydroxycarbamide(Hydroxy urea):

Plant derivatives: Vinca alkaloids: MOA: Binds to tubulin & inhibits its polymerization preventing spindle fobre formation during cell division & also inhibits leucocyte phagocytosis, chemotaxis and also axonal myelotoxicity Taxanes: Ex:Paclitaxel,Docetaxel MOA:

They act on microtubules stabilizing them in polymerized state Paclitaxel is given by I.V. infusion Docetaxel is given Orally Used in combination with carboplatin , paclitaxel is used in ovarian cancer Corticosteroids & antihistamines pretreatment is necessary for Taxane therapy Inhibits mitochondrial function & nucleoside transport Inhibits Topoisomerase II Ex:Irinotecan,topotecan Inhibits Topoisomerase I These alkaloids have fewer side effects compared with other anticancer drugs

Etoposides:

Campothecins:

Hormones: i)Glucocorticoids:

Ex:Prednisolone, hexamethasone Inhibits lymphocyte proliferation Used in the treatment of leukaemias & lymphomas Ex:Diethylstilbestrol,ethinyloestradiol Used for the treatment of androgen dependent prostrate cancer Prostrate cancer can also be treated with gonadotropin releasing hormone analogues Ex:medroxy progesterone, megestrol Used for the treatment of endometrial neoplasm and renal cancer Ex:goserelin, buserelin Used for the treatment of breast cancer in post menopausal women & prostrate cancer Ex:Octreotide, lanreotide

Estogens:

Progestrogens:

Gonadotrophin-releasing hormone analogues:

Analogues of somatostatin:

19

Used for the treatment of neuro endocrine tumours

Hormone anatagonists: Antioestrogens

Ex:Tamoxifen Used for the treatment of breast cancer It has cardioprotective activity by inhibiting LDL Ex:Anastrozole, letrozole Used for treatment of breast cancer Aminoglutethimide blocks the generation of all steroids Ex:Flutamide, bicalutamide, ciproterone Used in the treatment of prostrate cancer Ex:Trilostrane,Aminoglutethimide Used to inhibit early stages of sex hormone synthesis

Aromatase inhibitors:

Antiandrogens:

Adrenal hormone synthesis inhibitors:

Radio active isotopes: Ex: I131 used for treatment of thyroid cancer Cisantaspase: It is the preparation of an enzyme asperginase Adverse effect: Anaphylactic shock Monoclonal antibodies: Ex:trastuzumab,rituximab Rituximab:

licensed for the treatment of lymphoma It lyses B-lymphocytes by binding to Ca+ channel forming CD-20 protein & activating the complement.

Unwanted effects: Hypotension Trastuzumab:

Is a humanized murine mab that binds to a protein termed HER2(Human epidermal growth factor receptor) Inhibitor of signaling pathway kinases It inhibits not only platelet-derived growth factor but also a cytoplasmic kinase Inhibits RAS pathway

Imatinib mesylate:

Biological response modifiers: Ex:Aldesleukin(recombinant interleukin 2) The other drugs used are Tyrosine kinase inhibitors, angiogenesis & metalo proteinase inhibitors, cycloxigenase inhibitors, P53 in the another target, antigen oligo nucleotides & gene therapy ANTI PROTOZOALS: Anti malarials:

P.falciparum P.malariae

-produces malignant tertian malaria

P.falciparum -no exo-erythrocytic cycle P.vivax - benign tertian malaria

20

P.0vale

P.malariae- quartan malaria

Drugs used to treat acute attack/blood schizonticidal drugs: They act on erythrocytic forms of the plasmodium 1.Quinoline-methanols Ex:Quinine,Mefloquine 2.4-aminoquinolines Ex:Chloroquine 3.phenanthrene deriv.: Halofantrine 4.Drugs inferring with folate synthesis: Sulfones 5. Drugs inferring with action of folate : Ex:Pyrimethamine, Proguanil 6.Naphtoquinone derive.: Atovaquone 7.Antibiotics: Tetracyclines(Broad spectrum) Used in losa losa fever 8.Compounds derived from qinghaosu: Artemether, arteflene, artesunate Drugs that effect a radical cure(root level): Tissue schizonticidal drugs Ex:8-amino quinolines : Primaquine and tafenoquine They mainly act on liver parasites Drugs used for chemophylaxis(causal prophylactic drugs): They block the link between exoerythrocytic cycle and erythrocytic cycle Ex:Chloroquine, mefloquine, proguanil, pyrimethamine, dapsone and doxycycline Drugs used to prevent transmission: They have gametocidal action Ex: proguanil, pyrimethamine, priaquine 4-amino quinolines: i)Chloroquine:

It is the most potent blood-schizonticidal agent It is effective against all 4 forms of plasmodium sps. At high concentrations it inhibits protein, DNA ,RNA synthesis(this is not related to antimalarial activity) It inhibits haeme polymerase enzyme in parasite Chloroquine is used as disease modifying antirheumatoid drug Unwanted effects:
o o

In higher doses it causes retinopathy It has quinidine like action on heart

Note:Chloroquine can be considered as safe drug for pregnant women Quinoline methanols: Quinine:
o o o o o o

It is an alkaloid derived from cinchona bark It is effective against erythrocytic forms on 4 forms of plasmodium but has no effect on exo erythrocytic forms It inhibits haeme polymerase It is the main chemotherapeutic agent for p.falciparum It has a mild oxytocic effect on uterus It also has neuromuscular & antipyretic activity

21

Unwanted effects:
o o o

Cinchonism It causes hypertension by increasing synthesis of insulin Rarely it causes black water fever a fatal condition associated with haemolytic anaemia and renal failure Blood schizonticidal quinoline-methanol p.falciparum and p.vivax It is used in combination with pyrimethamine It also inhibits haeme polymerase Its plasma halflife is 30days compound active against

Mefloquine:
o o o o

Unwanted effects: CNS toxicity-insomnia, psychosis, dizziness Note:Contraindicated in pregnant women due to its long plasma half life Phenanthrene-methanols: Halofantrine:
o o o

It is a blood-schizonticidal agent It is active against strains of p.falciparum that are resistant to chloroquine, pyrimethamine, quinine It is effective against P.vivax It can cause severe cardiac dysrhythmia It prolongs QT interval Cough Haemolytic anaemia Type I : Sulfonamides & sulfones They mainly act by competing with TypeII : Pyrimethamine & Proguanil They inhibit dihydrofolate reductase Type I + Type II = Synergistic action Pyrimethamine is a 2,4-diaminopyrimidine and it is used only in combination with dapsone & sulfonamide Sulfodoxine is mainly used sulfonamide in malaria Pyrimethamine+sulfodoxine = used in chloroquine resistant malaria The active form of proguanil is cycloguanilproguanil has inhibitory blood schizonticidal activity Pyrimethamine+dapsone: eosinophilic alveolitis haemolytic anaemia, agranulocytosis, and PABA

Unwanted effects:
o o o o

Drugs affecting the synthesis or utilization of folate:

o o o o o o o o o

Unwanted effects:
o o o

Pyrimethamine+sulfadoxine:blood dyscariasis, allergic alveolitis Pyrimethamine causes megaloblastic anaemia

8-aminoquinolines: Ex:Primaquine, etaquine, tafenoquine

o o

Primaquine has little effect on erythrocytic state Tafenoquine is long acting

Unwanted effects: 22

o o o

Methaemoglobinaemia with cyanosis Haemolysis in individuals with an x-chromosome-linked genetic metabolic condition-glucose 6 phosphate dehydrogenase deficiency Primaquine metabolites have greater haemolytic activity than parent drug

Antibiotics: Tetracycline & doxycycline Artemisinin:

o o o o o

Drug of choice in cerebral malaria It has an endoperoxide linkage Artesunate is water soluble derivative of artemisinin Mechanism of action is mainly due to damage to DNA by generating free radicals The active form of artemisinin is dihydroartemisinin It causes decrease in neutrophil count Transient heart block It disturbs auditory functions

Unwanted effects:
o o o

Artemisinin potentiates the effects of mefloquine, primaquine & tetracyclines Artemisinin anatagonises the actionsw of the sulfonamides & the folate antagonists Artemether and lumefantrine are used in combination Hydroxy napthaquinine derivatives: Atovaquone mimics the actions ofubiquinone possibly mitochondrial electron transport chain in the parasite Atovaquone + proguanil = SYNEGISM New antimalarial drugs: Pyonaridine is currently used in china It is effective against xhloroquine resistant p.falciparum DRUGS USED IN TOXOPLASMOSIS: Causative organism: Toxoplasma conidia Treatment:
o o o o

by

inhibiting

the

Pyrimethamine + sulfadiazine(to be avoided in pregnant patients) Trimethoprim + sulfamethaxazole Parenteral pentamidine Azithromycin is also used

CILIATE INFECTIONS: Causative organism: pneumocystis carinii Treatment:

o o o o

High doses of co-trimaxazole is the drug of choice Parenteral pentamidine Trimethoprim + Dapsone Atovaquone/Clindamycin + primaquine

TRICHOMONIASIS: Causative organism:Trichomonas vaginalis Treatment:

o o

Metranidazole High doses of Tinidazole

23

GIARDIASIS: Causative organism: Giardia lamblia Metronidazole is the drug of choice AMOEBIASIS: Causative organism:Entamoeba histolytica Treatment:
o o o o

Metronidazole(or tinidazole) followed by diloxanide for acute invasive intestinal amoebiasis Diloxanide for chronic intestinal amoebiasis Metronidazole followed by diloxanide for hepatic amoebiasis Diloxanide for the carrier state It kills the trophozoites of E.histolytica but has no effect on cysts It acts by promoting apoptosis in the parasite The drug has a metallic bitter taste It interferes with alcohol metabolism so concurrent use of it is strictly avoided This drug is contraindicated in pregnant women

Metronidazole:
o o

Unwanted effects:
o o o

Tinidazole also has the similar action but longer acting Diloxamide:
o o

These drugs are used for the asymptomatic patients They show direct amoebicidal activity

TRYPANOSOMIASIS: Causative organism: Trypanosoma gambiense Trypanosoma rhodesiense which causes sleeping sickness in Africa Trypanosoma cruzi which causes chagas disease in South America Treatment: Drugs for sleeping sickness:
o o o

Suramin, pentamidine(haemolymphatic stage) Arsenical melarsoprol for late stage with CNS involvement Other agents: nifurtimox(chagas disease), eflornithine

Suramin: MOA: It doesnot kill the parasite immediately but inhibits parasites enzyme inducing gradual destruction of organelles Unwanted effects:
o o o o o

Nephrotoxicity Should not be given to malnourished patients Optic atrophy Adrenal insufficiency Haemolytic anaemia It has a direct trypanocidal action It directly interacts with DNA It doesnot cross BBB

Pentamidine isethionate:
o o o

24

Unanted effects:
o o o

Immediate hypotension followed by reflex tachycardia Breathlessnesss Kidney damage

LEISHMANIASIS: Causative organism: Leishmania sps Treatment: The main drugs used are sodium stibogluconate, meglumine antimoniate, pentamidine isethionate, miltefosine
o o

Miltefosine(hexadecylphosphocholine) is effective in treating cutaneous and visceral leishmaniasis sodium stibogluconate hypotension its main unwanted effects are bradycardia,

MOA: its main action is by increasing production of oxygen free radicals which are toxic to the parasite DIURETICS Classification: i)Diuretics acting on proximal tubule: loop diuretics ii)Diuretics acting on distal tubule: thiazide diuretics Aldosterone antagonists iii)Diuretics acting indirectly: osmotic diuretics Loop diuretics:
o o o o o o o o

Loop diuretics are the most powerful diuretics MOA:they inhibit the Na+/K+/2cl- carrier in the lumenal membrane These are also called as high ceiling diuretics They are sulfomoyl derivatives Ex:Furosimide, bumetanide,Toresamide, organomercurials(mersalyl) Ethacrynic acid,

They increase excretion of calcium and magnesium and decrease excretion of uric acid(promotes gout) Thiazide diuretics: reduce excretion of calcium ions Loop diuretics are contraindicated in older woman Hypotension Hypovolemika Hypokalemia Metabolic alkalosis

Unwanted effects:
o o o o

Note: Loop diuretics precipitates gout Ethacrynic acid:when given with aminoglycosides it causes ototoxicity Clinical uses:
o o

Drug of choice in CHF It is used for the treatment of hypertension complicated with renal impairment

25

Hypokalemia increases toxicity of digoxin & type III antidysrhythmic drugs Ex:Bendroflumethazide, metolazone hydrochlorothiazide, chlortalidone, indapamide,

Drugs acting on distal tubule:

o o o o o o o o o o o

Metolazone doesnot contain any thiazide nucleus MOA: it inhibits Na-cl transporter system Increases potassium & magnesium loss from the body Decrease uric acid secretion & also calcium excretion Thiazides are preferred over loop diuretics in term sof bone metabolism during long turn usage of older patients Loop diuretics +thiazide diuretics = synergism Thiazide diuretics cause hyperglycemia Diazoxide a non diuretic thiazide causes vasodilation by activating KATP channels They oppose the actions of oral sulfonyl ureas such as glibenclamide This diuretic can also be used in Diabetes insipidus

Pharmacokinetics: Chlorpthalidone longer acting thiazide diuretic acting on distal tubule Uses:
o o o o

Used in nephrogenic insipidus Chlorpropamide used in neurogenic diabetes insipidus Metolazone especially used with loop diuretics It is used in recurrent stone formation in idiopathic hypercalciuria Gitelmans syndrome due to inactivation of Na+/cl- cotransporter in the distal tubule Metabolic alkalosis Hypokalaemia Hypocalciuria may be beneficial as regards to bone metabolism and stone formation Erectile dysfunction seen with thiazide diuretics but reversible It precipitates gout & diabetes

Unwanted effects:
o o o o o o

Aldostreone antagonists: Spiranolactone, Eplerenone

o o o o o

MOA: it inhibits aldosterone activity Eplerenone differs from spiranolactone by replacement of 17-thio acetyl group with a carbomethoxy group Plasma half life of spiranolactone is 10minutes Active metabolite of spiranolactone is canrenone (active) t1/2 = 16hrs Hyperkalemia Metabolic acidosis Gynaecomastia Menstrual disorders Testicular dystrophy

Unwanted effects:
o o o o o

Eplerenone has lower oestrogen like activities than spiranolactone 26

Uses:
o o o

It is used along with digoxin for treatment of CHF Can inhibit cardiac remodeling Used in conns syndrome(hyper aldosteronism)

Triamterene and amiloride: MOA: it blocks Na+ absorption in distal tubule Unwanted effects: metabolic acidosis Triamterine is guanidine containing diuretic it is seen in kidney stones Diuretics that act indirectly:
o o o

Osmotic diuretics: given by IV route Ex: mannitol They are not useful in treating conditions of heart failure associated with Na retention But can be used in emergencies for treating acutely raised intracranial & intraocular pressure Expands extracellular fluid volume with a risk of causing left ventricular failure Hyponatraemia Citrate:inhibits carbonic anhydrase enzyme having antibacterial activity Barbiturate poisoning can alkalinize the urine by NaHCO3(used to treat salicylic acid overdose)

Unwanted effects:
o o

Drugs that alter pH of urine:

o o

Drugs that decrease urinary pH :NH4cl Diuretics that act indirectly: Acetazolamide used in infantile epilepsy Increases pH of urine and causes metabolic acidosis Used in glaucoma
o

Ethanol inhibits the secretion of ADH causing water dieresis and inhibition of transient diabetes insipidus Lithium used in psychiatric disorder Demeclocycline- a tetracycline used not as an antibioticused in ling cancers with inappropriate ADH secretion Colchicines & vinca alkaloids cause nephrogenic dibetes insipidus

Drugs that inhibit action of ADH:

o o o

Nephrogenic diabetes insipidus: diabetes insipidus caused not by a failure to secrete ADH but by a failure of the renal collecting ducts to respond to its action Hyperkalaemia:
o o o o o

Treatment neede if plasma concentration exceeds 6.5m mol/l Calcium gluconate is given by IV Salbutamol(albuterol) causes cellular K+ uptake Salbutamol + insulin = synergism Removal of excessive potassium from the body can be achieved by cation exchange resins such as sodium or calcium polystyrene sulfonate(sorbitol is given in combination to prevent constipation)

Drugs used in urinary tract infections: Bed wetting(enuresis) is treated by v2 selective (ADH receptor) Desmopressin (oral or nasal) restricting fluid intake TCA(amitryptiline) but has side effects 27

Benign prostatic hypertrophy antiandrogen 5- reductase inhibitor (finasteride 1 antagonist terazosin ,tamsulosin doxazocin Urinary incontinence: M3 antagonists darifenacin, Oxybutinin. Tolteridone Hyperphosphataemia: Drugs used Antacid-Al(OH)3(but increase plasma Al) The use of alum as a water purifier led to dialysis dementia Ca-containing phosphate binding agent(CaCO3) is used An anion exchange resin sevelamer lowers plasma phosphate (contraindicated in bowel obstruction) NOTES:wagners granulomatosis cause renal failure
o o

immunosuppressant drugs are used for this syndrome vit-D preparations(calcitrol & alphacalcidol) are used to treat osteodystrophy of chronic renal failure, 2) pagets disease of bone is treated by calcitonin

28