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Tranq,sed,hypnotic
pharmacology
| Question | Answer |
|---|---|
| Agents- depress central nervous system which enables the animal to go to sleep more easily. e.g. Chloral Hydrate. | Hypnotic |
| Drugs which relives anxiety and results in - easer for patient to rest or sleep. | Sedative |
| These drugs causes drowsiness. | Sedative |
| Xylazine is more like | sedative |
| Predominant action of these drugs is in relieving anxiety without producing undue sleep. They affect mood and behavior | Tranquilizer (Ataractic) |
| Some times these three categories are classified, based on medical-clinical uses. | Antianxiety: (older terminology “ Neuroleptics”) Antipsychotic: Sedative/ Hypnotic |
| Drugs which reduce psychomotor agitation, curiosity, and aggressiveness exert their effects by blocking | dopamine mediated responses in the central nervous system (CNS |
| Phenothiazine and Butyrophenone.. they are now categorized as | antipsychotic drugs. |
| are used for premedication but they will not quieten the animal and may be more difficult to handle by removing inhibition. So that the vicious animal become more likely to bite or kick. | Benzodiazepines: |
| Classification | Phenothiazines. II. Butyrophenone. III. Benzodiazepines.IV. Alpha-2- Adrenoceptor Agonist.V. Analgesic drugs. (i). NonsteroidsVI. Opioid Analgesics |
| Phenothiazine Tranquilizers | Acepromazine.Promazine.ChlorpromazinePropriopromazine.Triflupromazine.MethotrimeprazinePromethazine |
| They are dopamine antagonist, having calming and mood altering effects. They can increase the rate of turnover (synthesis and destruction) in the brain. They also increase turnover of norepinephrine | Phenothiazine Tranquilizers |
| This group is classified as antipsychotic agent and have wide range of central and peripheral effects., but the degree of activity varies | Phenothiazine Tranquilizers |
| Powerful antiemetic. | Phenothiazine Tranquilizers |
| In general they do not have analgesic activity. | Phenothiazine Tranquilizers |
| Alpha-1-adrenoceptor blocker, can cause hypotension | Phenothiazine Derivatives |
| Has antiarrhythmic effect on heart | Phenothiazine Derivatives |
| Has spasmolytic action on the gut, in horse gut motility is not reduced | Phenothiazine Derivatives |
| Varying degree of antihistamine activity. | Phenothiazine Derivatives |
| May cause hypothermia: It acts on CNS thermoregulation center to drop body temperature | Phenothiazine Derivatives |
| FDA approved for dog, cat and horse. | Acepromazine |
| Can be given, I/V, I/M and subcutaneous | Acepromazine |
| Oral doses can also be used | Acepromazine |
| Possesses antiemetic, anticonvulsant, antispasmodic, hypotension and hypothermic properties | Acepromazine |
| Lowers the convulsive seizure threshold thus contraindicated seizure cases | Acepromazine |
| May prevent malignant hyperthermia syndrome in susceptible pig exposed to halothane | Acepromazine |
| Decreases PCV | Acepromazine |
| Not to use with organophosphate compounds, may cause seizure activity | Acepromazine |
| In horse it may cause priapism, thus not to use in stallion | Acepromazine |
| In halothane anesthesia, epinephrine induced ventricular arrhythmias and fibrillation can be prevented | Acepromazine |
| Increase doses does not increase tranquilization. May even cause excitement | Acepromazine |
| Widely used in Europe | Propionylpromazine |
| Less potent than acepromazine. Had unreliable action in horses. Mostly used in human subjects. | Chlorpromazine |
| Action similar to acepromazine. Has better sedative effect than chlorpromazine | Promazine |
| Is a typical phenothiazine but it is also a potent analgesic, having a potency about 0.7 times that of morphine | Methotrimeprazine |
| Is mostly used as antihistamine | Promethazine |
| Butyrophenone Derivatives | Azaperone, Droperidol and Fluanisone |
| class of drugs causes tranquilization and sedation, anti-emetics, reduce motor activity and inhibits CNS catecholamines (dopamine, norepinephrine). | butyrophenone |
| Not marketed in USA | Azaperone |
| Mostly used in pigs in other countries. | Azaperone |
| Has been effective in halothane induced malignant hyperthermia in susceptible pigs | Azaperone |
| . Its effects can be antagonized by 4-aminopyridine. Duration of action 2 to 3 hours. | Azaperone |
| Used for control of aggressiveness when mixing or regrouping the pigs. Metabolized by liver | Azaperone |
| Is along acting (6-8 hours), potent neuroleptic. Its use is approved in dogs. | Droperidol |
| The principal use has been as a compound of Innovar-Vet in mixture with fentanyl. This combination produces neuroleptic-analgesia | Droperidol |
| Was used in 70’s and 80’s, but no longer marketed | Droperidol |
| This combination produces neuroleptic-analgesia | compound of Innovar-Vet in mixture with fentanyl |
| These agent are used for their central (CNS) effect of profound sedation and analgesia | Alpha-2 Adrenergic Agonists |
| CNS depression is mediated by stimulation (activation) of alpha-2-adrenoceptrs | Alpha-2 Adrenergic Agonists |
| Even at sub-sedative doses, analgesia occurs through both spinal and central action | Alpha-2 Adrenergic Agonists |
| share similar regions of the brain | Opioid and Alpha-2-adrenoceptors |
| The locus ceruleus (located in ventral medulla) in brain is believed to be the major site of action for | alpha-2-sedatives. |
| Alpha-2-adernergic Agonist Sedation: Primary action is mediated by activation of alpha-2-adrenoceptors They serve as | prejunctional inhibitory receptors (autorecptor) with in the sympathetic nervous system. |
| Alpha-2-adernergic Agonist Muscle relaxant activity is caused by/ | inhibition of intraneural transmission with in CNS system |
| Alpha-2-adernergic Agonist CNS effects: Anticonvulsant and also may be effective in cases of | opioid withdrawal syndrome. |
| Alpha-2-adrenoceptors Agonist Systemic Effects: | GI tract, uterus, kidney, platelets and verity of other effects |
| Alpha-2-adrenoceptors Agonist Peripheral Effects: | Hypertension: Post-synaptic alpha-1 and -2. Hypotension: Mediated via CNS causing decreased sympathetic out flow by activation of pre-synaptic alpha-2 |
| Alpha-2-adrenoceptors Agonist Cardio-Pulmonary effects: | A-V block, decrease heart rate by enhancing vagal tone. pulmonary effect: Depress respiratory center in medulla etc.. |
| Alpha-2-adenoceptors Agonists: | Xylazine.Detomidine.Medetomine.Romifidine |
| Alpha-2-adenoceptors Antagonists: | YohimbineTolazolineIodazoxan.Atipamezole |
| Is approved by FDA for dog, cat and horse. Not approved for ruminants | Xylazine |
| Can be used in combination with other drugs. | Xylazine |
| Half life; Sheep = 23 min., Dog = 30 min. Cattle =36 min., and horse =50 min | Xylazine |
| Duration of action: 15-30 min. Also dose dependent | Xylazine |
| Can be given IV, IM, S/C. | Xylazine |
| Cattle more sensitive than other animals | Xylazine |
| Cardio-vascular and respiratory depression. HR , CO, BP, Resp | Xylazine |
| Horse may respond with well directed kick (Kick response) due to sudden touch. | Xylazine |
| Horse: Violent excitement (IV), sudden death and collapse. May be intra-carotid injection | Xylazine |
| Vomiting in dog and cat | Xylazine |
| Hyperglycemia. | Xylazine |
| Urine production increases. Anti-ADH effect. | Xylazine |
| Uterine contraction: May cause abortion in cow in last trimester of pregnancy | Xylazine |
| May cause anaphylactic shock | Xylazine |
| Used as premedication for sedation and analgesia. | Xylazine |
| Can be used for epidural anesthesia. | Xylazine |
| Xylazine Metabolized by | liver and excreted by kidney |
| Xylazine Precaution and Contraindications; | Heart condition,Liver and renal impairment,Can cause hypothermia in cold temperature,May also cause hyperthermia in hot summer in Alabama due to depression of respiratory center,causing decreased respiration,Shock and dehydration.Epilepsy. |
| Developed for horses and cattle | Detomidine (Dormosedan) |
| Has higher potency and greater specificity at central alpha-2-adrenoceptros | Detomidine (Dormosedan) |
| Cardiovascular effects similar to xylazine. | Detomidine (Dormosedan) |
| Sedation last for 90 to 120 min. | Detomidine (Dormosedan) |
| Pain relief for 75 to 80 min. Used in equine colic cases. | Detomidine (Dormosedan) |
| Do NOT have ecbolic effect in cattle | Detomidine (Dormosedan) |
| Other effects are similar to xylazine | Detomidine (Dormosedan) |
| Is most potent alpha-2-adrenoceptor agent. | Medetomidine |
| Sedation, analgesia, muscle relaxation occurs in variety of domestic animals | Medetomidine |
| Selectivity binding ratio for: alpha-2 / alpha-1.Medetomidine Detomidine Clonidine Xylazine | 1620, 260, 220, 160 |
| In dogs and cats it produces. Dose dependent sedation and analgesia | Medetomidine |
| Where as with xylazine and detomidine, higher doses may not result in more sedation, but increase in duration of action. | Medetomidine |
| Drug is used as premedication before induction of anesthesia .. In combination with other drugs | Medetomidine |
| Horse: Produces more ataxia and disorientation, thus not preferred | Medetomidine |
| Primarily used in dog and cats | Medetomidine |
| Contra indications are: Similar to xylazine and other drugs in this group | Medetomidine |
| Pharmacokinetics: Onset of action is rapid (5min) with IV and 10 to 15 min with IM injections | Medetomidine |
| Drug not recommended for use in pregnant dogs | Medetomidine |
| It is safe to use with opioids, Benz diazepam and other anesthetics | Medetomidine |
| This drug, developed from clonidine, has typical alpha-2-adrenoceptor against effect | Romifidine |
| Used thus far in horses as sedative and premedication | Romifidine |
| Produces less ataxia and head in not lowered at the same extent | Romifidine |
| Duration of action is longer than the others | Romifidine |
| Horse remains quieter than normal for considerable time after obvious sedation has waned. Causes marked urination in about 90 min. | Romifidine |
| Maximal Sedative IV doses in horse are: Romifidine Xylazine Detomidine | Romifidine 80 ug/kgXylazine 1mg/kgDetomidine 20 ug/kg. |
| Alpha-2-Adrenoceptor Antagonists are | Yohimbine.Iodazoxan.Tolazoline.Atipamezole |
| is not Alpha-2- Adrenoceptor antagonists, but causes release of acetylcholine and other neurotransmitters from CNS pre-synaptic nerve endings. Thus has been used to reverse the action of some the alpha-2- agonists | *** 4-aminopyridine |
| Is very effective alpha-2-antagonists | Yohimbine |
| It reverses sedation and analgesia in many animal species | Yohimbine |
| Is a Rauwolfia or indolealkylamine of alkaloid. It is chemically related to reserpine | Yohimbine |
| Action is alpha-2 adrenoceptor mediated depression (blocking central alpha-2 receptors) thus enhance norepinephrine release and increase sympathetic out flow | Yohimbine |
| It penetrate CNS quite readily, reversal of xylazine occurs in 3 min | Yohimbine |
| Alpha-adrenergic blocker and structurally related to phentolamine | Tolazoline (Priscoline) |
| Possesses the least specificity for alpha-2-adrenoceptor than all other antagonists in this group | Tolazoline (Priscoline) |
| Is approved for xylazine reversal in horse. | Tolazoline (Priscoline) |
| Given IV rapid action is in 5 min | Tolazoline (Priscoline) |
| It is also a competitive alpha 1 and alpha 2 adrenergic blocker, thus has peripheral vasodilation | Tolazoline (Priscoline) |
| Anti-sedative effect is far superior than other drugs in this group | Atipamezole |
| Alpha 2/ alpha 1, selective ratio of atipamezole is 200 to 300 times higher than idazoxan or yohimbine. | Atipamezole |
| Is an alpha 2- adrenergic antagonist | Atipamezole |
| Its labeled for use as medetomidine reversal agent. | Atipamezole |
| Some animal have died following rapid IV of high doses | Atipamezole |
| Not recommended in pregnant and lactating animal | Atipamezole |
| a purine alkyl piperidine derivative has been used in clinical investigation in cattle for its sedative effects | Tameridone |
| Has been tried for the capture and transport of wild ruminants | Tameridone |
| It’s a sedative drugs but details NOT known | Tameridone |
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alljacks
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